Structure

InChI Key MYSWGUAQZAJSOK-UHFFFAOYSA-N
Smiles O=C(O)c1cn(C2CC2)c2cc(N3CCNCC3)c(F)cc2c1=O
InChI
InChI=1S/C17H18FN3O3/c18-13-7-11-14(8-15(13)20-5-3-19-4-6-20)21(10-1-2-10)9-12(16(11)22)17(23)24/h7-10,19H,1-6H2,(H,23,24)

Physicochemical Descriptors

Property Name Value
Molecular Formula C17H18FN3O3
Molecular Weight 331.35
AlogP 1.58
Hydrogen Bond Acceptor 5.0
Hydrogen Bond Donor 2.0
Number of Rotational Bond 3.0
Polar Surface Area 74.57
Molecular species ZWITTERION
Aromatic Rings 2.0
Heavy Atoms 24.0

Bioactivity

Mechanism of Action Action Reference
Bacterial DNA gyrase inhibitor INHIBITOR FDA
Assay Description Organism Bioactivity Reference
Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity) None 380.0 ug.mL-1 Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity) None 380.0 ug.mL-1 Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity) None 380.0 ug.mL-1
Compound evaluated in vitro for the ability to inhibit gyrase. None 5.3 ug.mL-1
Inhibitory activity against DNA gyrase enzyme was determined by supercoiling assay with Escherichia coli DNA gyrase Escherichia coli 500.0 nM
Inhibition of the gyrase mediated cleavage of supercoiled DNA Escherichia coli 5.3 ug.mL-1
Effect on replication DNA biosynthesis in Escherichia coli H560 (permeabilised cells) Escherichia coli 0.3 ug.mL-1
Supercoiling inhibition assay using purified DNA gyrase isolated from Escherichia coli H560 Escherichia coli 0.9 ug.mL-1
Inhibitory activity against gyrase supercoiling activity from Escherichia coli Escherichia coli 0.68 ug.mL-1
Inhibitory activity on replicative DNA biosynthesis in Escherichia coli H560 (permeabilised cells) Escherichia coli 0.3 ug.mL-1
Inhibition of [3H]muscimol binding to GABA A receptor 4-biphenylacetic acid at 10 e-4 M None 410.0 nM
Inhibitory concentration in supercoiling inhibition Escherichia coli DNA gyrase assay Escherichia coli 5.3 ug.mL-1
50% inhibitory concentration against DNA-gyrase Escherichia coli 5.3 ug.mL-1
Gyrase inhibitory activity against Escherichia coli Escherichia coli 0.3 ug.mL-1
Inhibition of Quinolone resistant gyrase Supercoiling Activity in Escherichia coli Escherichia coli 102.4 ug.mL-1
Inhibition of Wild Type DNA gyrase Supercoiling Activity in Escherichia coli Escherichia coli 1.6 ug.mL-1
Inhibitory effect against Escherichia coli Gyrase in Supercoiling assay Escherichia coli 0.68 ug.mL-1
Cytotoxicity was determined for the compound in HepG2 cell line Homo sapiens 37.47 ug.mL-1
Inhibitory concentration against Mycobacterium intracellular Mycobacterium intracellulare 0.25 ug.mL-1
Inhibitory concentration against Staphylococcus aureus; Not active Staphylococcus aureus 0.1 ug.mL-1
Inhibitory concentration against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Inhibitory activity against HeLa cell Topoisomerase II None 30.0 nM
Clonogenic cytotoxicity against Hamster V-79 cells Cricetulus griseus 200.0 ug.mL-1
Clonogenic cytotoxicity against Chinese hamster V-79 cells Cricetulus griseus 320.0 ug.mL-1
Cytotoxicity was determined for the compound in V79-4 cell line Cricetulus griseus 58.55 ug.mL-1
Inhibition of supercoiling activity of DNA gyrase from Staphylococcus aureus ISP 794 Staphylococcus aureus 5.0 ug.mL-1
Inhibitory concentration against DNA gyrase of Staphylococcus aureus Staphylococcus aureus 20.1 ug.mL-1
Inhibition of supercoiling activity of topoisomerase IV from Staphylococcus aureus ISP 794; Range = 2.5-5 ug/mL Staphylococcus aureus 5.0 ug.mL-1
In vitro inhibitory concentration against DNA gyrase from Escherichia coli H560 Escherichia coli 3.1 ug.mL-1
Antimycobacterial activity of compound against Mycobacterium tuberculosis H37Rv at 2 ug/mL Mycobacterium tuberculosis 95.0 %
Inhibition of DNA gyrase supercoiling in Escherichia coli ATCC 25922 Escherichia coli 300.0 nM
Inhibition of Bacillus subtilis topoisomerase4 activity Bacillus subtilis 1.9 ug.mL-1
Inhibition of Bacillus subtilis gyrase activity Bacillus subtilis 0.74 ug.mL-1
Inhibitory activity against wild type Escherichia coli gyrase Escherichia coli 300.0 nM
Inhibition of Escherichia coli gyrase Escherichia coli 200.0 nM
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs Homo sapiens 170.0 ug.mL-1
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs Homo sapiens 400.0 ug.mL-1
Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs Homo sapiens 160.0 ug.mL-1
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs Homo sapiens 150.0 ug.mL-1
Antiproliferative effect against HeLa cells after 48 hrs Homo sapiens 290.0 ug.mL-1
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs Homo sapiens 120.0 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 18 to 24 hrs Staphylococcus aureus 0.09 ug.mL-1
Antibacterial activity against Mycobacterium intracellular ATCC 23068 after 68 to 72 hrs Mycobacterium intracellulare 0.3 ug.mL-1
Antibacterial activity against Mycobacterium intracellular ATCC 23068 Mycobacterium intracellulare 0.35 ug.mL-1
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv Mycobacterium tuberculosis 10.0 ug.mL-1
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 6.25 ug/mL Mycobacterium tuberculosis 98.0 %
Antimicrobial activity against Mycobacterium intracellular ATCC 23068 Mycobacterium intracellulare 420.0 nM
Inhibition of Escherichia coli H560 DNA gyrase assessed as DNA cleavage Escherichia coli 400.0 nM
Antibacterial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.08 ug.mL-1
Inhibition of Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as inhibition of pBR322 DNA supercoiling Mycobacterium leprae 3.5 ug.mL-1
Antimicrobial activity against Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against Mycobacterium intracellular Mycobacterium intracellulare 0.25 ug.mL-1
Antimicrobial activity against Staphylococcus aureus Staphylococcus aureus 0.07 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 Staphylococcus aureus 300.0 nM
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 Staphylococcus aureus 0.06 ug.mL-1
Antimicrobial activity against Mycobacterium intracellular ATCC 23068 Mycobacterium intracellulare 0.25 ug.mL-1
Inhibition of Escherichia coli DNA gyrase Escherichia coli 400.0 nM
Antimicrobial activity against Staphylococcus aureus ATCC 29213 by modified NCCLS method Staphylococcus aureus 0.15 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by modified NCCLS method Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against Mycobacterium intracellular by Alamar blue assay Mycobacterium intracellulare 0.45 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by antimicrobial susceptibility test Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against Mycobacterium intracellular ATCC 23068 by alamar blue method Mycobacterium intracellulare 0.4 ug.mL-1
Antibacterial activity against Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against Mycobacterium intracellular by alamar blue assay Mycobacterium intracellulare 0.25 ug.mL-1
Antifungal activity against Mycobacterium intracellular ATCC 23068 at 37 degC after 68 to 72 hrs Mycobacterium intracellulare 0.3 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 18 to 24 hrs Staphylococcus aureus 300.0 nM
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by NCCLS method Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against Mycobacterium intracellular ATCC 23068 by alamar blue assay Mycobacterium intracellulare 0.25 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 18 to 24 hrs by alamar blue assay Staphylococcus aureus 400.0 nM
Antibacterial activity against Staphylococcus aureus ATCC 29213 by alamar blue assay Staphylococcus aureus 400.0 nM
Antibacterial activity against Escherichia coli ATCC 35218 after 18 to 24 hrs by alamar blue assay Escherichia coli 10.0 nM
Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 Pseudomonas aeruginosa 1.18 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 by modified CLSI/NCCLS method Staphylococcus aureus 360.0 nM
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by modified CLSI/NCCLS method Staphylococcus aureus 360.0 nM
Antibacterial activity against Escherichia coli ATCC 35218 by modified CLSI/NCCLS method Escherichia coli 10.0 nM
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by modified CLSI/NCCLS method Pseudomonas aeruginosa 220.0 nM
Inhibition of Staphylococcus aureus wild type DNA topoisomerase 4 Staphylococcus aureus 1.24 ug.mL-1
Inhibition of Staphylococcus aureus DNA topoisomerase 4 Ser80Phe mutant Staphylococcus aureus 22.4 ug.mL-1
Inhibition of Staphylococcus aureus wild type DNA gyrase Staphylococcus aureus 13.4 ug.mL-1
Inhibition of Staphylococcus aureus DNA gyrase Ser84Leu mutant Staphylococcus aureus 256.0 ug.mL-1
Antimycobacterial activity against Mycobacterium intracellular ATCC 23068 Mycobacterium intracellulare 0.3 ug.mL-1
Antibacterial activity against Mycobacterium intracellular by after 4 days alamar blue assay Mycobacterium intracellulare 910.0 nM
Antibacterial activity against methicillin-resistant Staphylococcus aureus by NCCLS method Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against Staphylococcus aureus by NCCLS method Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against methicillin resistant Staphylococcus aureus ATCC 43300 Staphylococcus aureus 140.0 nM
Antimicrobial activity against methicillin resistant Mycobacterium intracellular ATCC 23068 Mycobacterium intracellulare 470.0 nM
Antimicrobial activity against Staphylococcus aureus ATCC 29213 by CLSI method Staphylococcus aureus 0.09 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by CLSI method Staphylococcus aureus 0.05 ug.mL-1
Inhibition of Escherichia coli DNA gyrase-mediated supercoiling of pBR322 using bromothymol blue by electrophoresis Escherichia coli 0.34 ug.mL-1
Inhibition of Escherichia coli DNA topoisomerase-4-mediated decatenation of pBR322 by electrophoresis Escherichia coli 4.6 ug.mL-1
Antibacterial activity against ciprofloxacin-resistant Salmonella enteritidis 104 harboring gyrA D87Y/S83F mutant, soxR R20H mutant and soxS E52K mutant gene assessed as reduction in swim motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 66.0 %
Antibacterial activity against ciprofloxacin-susceptibility revert strain of Salmonella enteritidis 104 harboring gyrA D87Y/S83F mutant, parC D79N mutant, soxR E16G/R20H mutant and soxS E52K mutant gene assessed as reduction in swim motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 90.0 %
Antibacterial activity against ciprofloxacin-resistant Salmonella enteritidis 5408 harboring gyrA D87Y mutant, gyrB E466D mutant, parE V461G mutant and ramR G25A mutant gene assessed as reduction in swim motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 93.0 %
Antibacterial activity against ciprofloxacin-resistant Salmonella enteritidis 104 harboring gyrA D87Y/S83F mutant, soxR R20H mutant and soxS E52K mutant gene assessed as reduction in swarm motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 36.0 %
Antibacterial activity against ciprofloxacin-resistant Salmonella enteritidis 5408 harboring gyrA D87Y mutant, gyrB E466D mutant, parE V461G mutant and ramR G25A mutant gene assessed as reduction in swarm motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 46.0 %
Antibacterial activity against ciprofloxacin-susceptibility revert strain of Salmonella enteritidis 104 harboring gyrA D87Y/S83F mutant, parC D79N mutant, soxR E16G/R20H mutant and soxS E52K mutant gene assessed as reduction in swarm motility after overnight incubation Salmonella enterica subsp. enterica serovar Enteritidis 36.0 %
Inhibition of reconstituted Escherichia coli DNA gyrase subunit AB assessed as reduction of DNA supercoiling activity using pBR322 DNA substrate Escherichia coli 300.0 nM
Inhibition of Escherichia coli DNA gyrase by gel electrophoresis Escherichia coli 100.0 nM
Inhibition of DNA supercoiling activity of Escherichia coli DNA gyrase Escherichia coli 450.0 nM
Inhibition of Escherichia coli DNA gyrase assessed as reduction of DNA supercoiling activity using pBR322 DNA substrate after 30 mins by electrophoresis Escherichia coli 0.34 ug.mL-1
Inhibition of Escherichia coli topoisomerase 4 assessed as decatenation of kDNA after 30 mins by electrophoresis Escherichia coli 4.6 ug.mL-1
Inhibition of Pseudomonas aeruginosa ATCC 27853 biofilm formation at 5 ug/ml after 24 hrs using crystal violet staining by spectrophotometry analysis Pseudomonas aeruginosa 51.0 %
Antibacterial activity against Staphylococcus aureus ATCC 29213 by NCCLS method Staphylococcus aureus 0.07 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by NCCLS method Staphylococcus aureus 0.07 ug.mL-1
Antibacterial activity against Escherichia coli by NCCLS method Escherichia coli 0.005 ug.mL-1
Antibacterial activity against Mycobacterium intracellular ATCC 23068 by alamar blue method Mycobacterium intracellulare 0.3 ug.mL-1
Inhibition of Escherichia coli DNA gyrase assessed as DNA supercoiling using pUC19 as substrate after 30 mins by agarose gel electrophoresis Escherichia coli 700.0 nM
Antimicrobial activity against Mycobacterium intracellular ATCC 23068 after 5 days by MABA assay Mycobacterium intracellulare 420.0 nM
Inhibition of Escherichia coli DNA gyrase-mediated supercoiling of relaxed pBR322 DNA Escherichia coli 800.0 nM
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 Plasmodium falciparum 8.82 ug.mL-1
Inhibition of DNA supercoiling activity of Escherichia coli DNA gyrase after 1 hr by agarose gel electrophoresis Escherichia coli 970.0 nM
Inhibition of DNA decatenation activity of Escherichia coli DNA topoisomerase 4 after 1 hr by agarose gel electrophoresis Escherichia coli 392.0 nM
Antimicrobial activity against Staphylococcus aureus ATCC 29213 by CLSI method Staphylococcus aureus 0.12 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by CLSI method Staphylococcus aureus 0.09 ug.mL-1
Antimicrobial activity against Mycobacterium intracellulare ATCC 23068 by Franzblau method Mycobacterium intracellulare 0.3 ug.mL-1
Antimicrobial activity against Escherichia coli ATCC 35218 by CLSI method Escherichia coli 0.003 ug.mL-1
Antimicrobial activity against Pseudomonas aeruginosa PAO1 assessed as inhibition of cell viability after 18 hrs by spectrophotometry Pseudomonas aeruginosa PAO1 38.0 nM
Inhibition of human ERG expressed in mammalian cells at 10 uM by patch clamp method Homo sapiens 1.0 %
Binding affinity to rat cerebral cortex histamine H3 receptor Rattus norvegicus 0.654 nM
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 Staphylococcus aureus 0.1 ug.mL-1
Antitubercular activity against Mycobacterium tuberculosis Mycobacterium tuberculosis 0.5 ug.mL-1
Antibacterial activity against Mycobacterium intracellulare ATCC 23068 assessed as growth inhibition after 70 to 74 hr by Alamar blue assay Mycobacterium intracellulare 0.32 ug.mL-1
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as growth inhibition after 16 to 20 hr by Alamar blue assay Pseudomonas aeruginosa 0.11 ug.mL-1
Antibacterial activity against Escherichia coli ATCC 35218 assessed as growth inhibition after 16 to 20 hr by Alamar blue assay Escherichia coli 0.005 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as growth inhibition after 16 to 20 hr by Alamar blue assay Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition after 16 to 20 hr by Alamar blue assay Staphylococcus aureus 0.11 ug.mL-1
Antimicrobial activity against Vibrio cholerae assessed as growth inhibition after 24 hr by cup-plate method Vibrio cholerae 200.0 nM
Antimicrobial activity against Pseudomonas aeruginosa NCIM 2967 assessed as growth inhibition after 24 hr by serial double dilution method Pseudomonas aeruginosa 50.0 nM
Antimicrobial activity against Escherichia coli NCIM 2068 assessed as growth inhibition after 24 hr by serial double dilution method Escherichia coli 30.0 nM
Inhibition of Mycobacterium leprae DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 2 hrs at 30 degC by ethidium bromide based gel electrophoresis Mycobacterium leprae 2.0 ug.mL-1
Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 1 hr at 37 degC by ethidium bromide based gel electrophoresis Mycobacterium tuberculosis 6.0 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by CLSI method Staphylococcus aureus 390.0 nM
Antibacterial activity against Staphylococcus aureus ATCC 29213 by CLSI method Staphylococcus aureus 390.0 nM
Inhibition of wild type Escherichia coli ATCC 25922 DNA gyrase subunit 2GyrA/2GyrB assessed as pBR322 supercoiling after 1 hr Escherichia coli 500.0 nM
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM Cricetulus griseus 105.26 %
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM Cricetulus griseus 112.43 %
Antimicrobial activity against Mycobacterium intracellulare ATCC 23068 by Alamar blue method Mycobacterium intracellulare 0.005 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by Alamar blue method Staphylococcus aureus 0.11 ug.mL-1
Antimicrobial activity against Staphylococcus aureus ATCC 29213 by Alamar blue method Staphylococcus aureus 0.14 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus by NCCLS method Staphylococcus aureus 390.0 nM
Antimicrobial activity against Staphylococcus aureus by NCCLS method Staphylococcus aureus 390.0 nM
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as growth inhibition after 16-20 hrs by CLSI method Staphylococcus aureus 0.09 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition after 16-20 hrs by CLSI method Staphylococcus aureus 0.08 ug.mL-1
Antibacterial activity against Staphylococcus aureus Staphylococcus aureus 0.12 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus Staphylococcus aureus 0.09 ug.mL-1
Antibacterial activity against Mycobacterium intracellulare Mycobacterium intracellulare 0.3 ug.mL-1
Antibacterial activity against Escherichia coli Escherichia coli 0.003 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by spectrophotometric analysis Staphylococcus aureus 0.3 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 after 24 hrs by spectrophotometric analysis Staphylococcus aureus 16.7 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by spectrophotometric analysis Staphylococcus aureus 16.7 ug.mL-1
Antibacterial activity against gentamicin-resistant Staphylococcus aureus ATCC 33592 after 24 hrs by spectrophotometric analysis Staphylococcus aureus 0.2 ug.mL-1
Antibacterial activity against Escherichia coli after 24 hrs by spectrophotometric analysis Escherichia coli 0.007 ug.mL-1
Antibacterial activity against Klebsiella pneumoniae after 24 hrs by spectrophotometric analysis Klebsiella pneumoniae 0.02 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 by CLSI method Staphylococcus aureus 0.08 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 16 to 20 hrs by CLSI method Staphylococcus aureus 0.09 ug.mL-1
Anti-biofilm activity against Staphylococcus aureus MTCC 96 assessed as inhibition of biofilm formation incubated for 24 hrs by crystal violet staining based modified biofilm inhibition assay Staphylococcus aureus 990.0 nM
Inhibition of Escherichia coli DNA gyrase using fluorescence-tagged DNA by fluorescenct polarization assay Escherichia coli 270.0 nM
Inhibition of Escherichia coli DNA gyrase assessed as supercoiled plasmid DNA formation after 30 mins by electrophoretic analysis Escherichia coli 200.0 nM
Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition Staphylococcus aureus 0.08 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as growth inhibition Staphylococcus aureus 0.09 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 Staphylococcus aureus 0.1 ug.mL-1
Antimicrobial activity against Staphylococcus aureus ATCC 29213 Staphylococcus aureus 0.1 ug.mL-1
Inhibition of Escherichia coli DNA gyrase after 1 hr by agarose gel electrophoresis Escherichia coli 150.0 nM
Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition using fresh sample in DMSO by CLSI method Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as growth inhibition using fresh sample in DMSO by CLSI method Staphylococcus aureus 0.1 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus EAMC30 assessed as growth inhibition using fresh sample in DMSO by CLSI method Staphylococcus aureus 29.4 ug.mL-1
Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as growth inhibition using fresh sample in DMSO by CLSI method Enterococcus faecalis ATCC 29212 0.2 ug.mL-1
Antibacterial activity against Enterococcus faecalis ATCC 51299 assessed as growth inhibition using fresh sample in DMSO by CLSI method Enterococcus faecalis 0.2 ug.mL-1
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 days by MTT assay Mycobacterium tuberculosis H37Rv 600.0 nM
Inhibition of Escherichia coli recombinant gyrase A2B2 assessed as reduction of pHOT-1 supercoiling after 90 mins Escherichia coli 460.0 nM
Inhibition of biofilm formation in Staphylococcus epidermidis ATCC 12228 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 7.0 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis ATCC 35984 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 11.59 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 16/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 6.81 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 23/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 42.76 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 24/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 12.95 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 31/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 22.13 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 62/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 4.81 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 63/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 7.14 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 76/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 7.93 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis 151/04 after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 13.1 ug.mL-1
Inhibition of biofilm formation in Staphylococcus epidermidis ATCC 12228 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 21.3 %
Inhibition of biofilm formation in Staphylococcus epidermidis ATCC 35984 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 45.43 %
Inhibition of biofilm formation in Staphylococcus epidermidis 16/04 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 41.96 %
Inhibition of biofilm formation in Staphylococcus epidermidis 23/04 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 5.71 %
Inhibition of biofilm formation in Staphylococcus epidermidis 31/04 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 18.66 %
Inhibition of biofilm formation in Staphylococcus epidermidis 62/04 at 4 ug/ml after 24 hrs using MTT staining by spectrophotometer analysis Staphylococcus epidermidis 59.89 %
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 0.2 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA1 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 10.4 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA2 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 2.9 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA3 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 4.4 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA4 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 2.0 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA5 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 5.3 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA6 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 2.5 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus CIMRSA7 after 18 to 24 hrs by spectrophotometric analysis Staphylococcus aureus 0.39 ug.mL-1
Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by spectrophotometric analysis Escherichia coli ATCC 25922 0.008 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS-16 MTCC 2940 after 24 hrs by crystal violet staining method Staphylococcus aureus 0.4 ug.mL-1
Antibiofilm activity against Escherichia coli MTCC 739 after 24 hrs by crystal violet staining method Escherichia coli 0.5 ug.mL-1
Antibiofilm activity against Micrococcus luteus MTCC 2470 after 24 hrs by crystal violet staining based method Micrococcus luteus 500.0 nM
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining based method Staphylococcus aureus 300.0 nM
Antibiofilm activity against Staphylococcus aureus MLS-16 MTCC 2940 after 24 hrs by crystal violet staining based method Staphylococcus aureus 400.0 nM
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by well diffusion assay by crystal violet staining based method Bacillus subtilis 500.0 nM
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining method Bacillus subtilis 0.7 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining method Staphylococcus aureus 0.6 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 0.6 ug.mL-1
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining based assay Bacillus subtilis 0.5 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 0.4 ug.mL-1
Antibiofilm activity against Micrococcus luteus MTCC 2470 after 24 hrs by crystal violet staining based assay Micrococcus luteus 0.6 ug.mL-1
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining based assay Bacillus subtilis 500.0 nM
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 700.0 nM
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 600.0 nM
Antibiofilm activity against Micrococcus luteus MTCC 2470 after 24 hrs by crystal violet staining based assay Micrococcus luteus 800.0 nM
Antibiofilm activity against Klebsiella planticola MTCC 530 after 24 hrs by crystal violet staining based assay Raoultella planticola 600.0 nM
Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 at 10 uM relative to control Mycobacterium tuberculosis H37Ra 99.7 %
Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 at 1 uM relative to control Mycobacterium tuberculosis H37Ra 99.6 %
Antibiofilm activity against Staphylococcus aureus MTCC 96 incubated for 24 hrs by crystal violet staining-based assay Staphylococcus aureus 0.6 ug.mL-1
Antibiofilm activity against Bacillus subtilis MTCC 121 incubated for 24 hrs by crystal violet staining-based assay Bacillus subtilis 0.5 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 incubated for 24 hrs by crystal violet staining-based assay Staphylococcus aureus 0.4 ug.mL-1
Antibiofilm activity against Micrococcus luteus MTCC 2470 incubated for 24 hrs by crystal violet staining-based assay Micrococcus luteus 0.4 ug.mL-1
Antimicrobial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method Staphylococcus aureus 300.0 nM
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by broth microdilution method Staphylococcus aureus 200.0 nM
Antibacterial activity against Enterococcus faecium DSM 20477 after 18 hrs Enterococcus faecium 2.29 ug.mL-1
Antibacterial activity against Escherichia coli DSM 1116 after 18 hrs Escherichia coli 0.01 ug.mL-1
Antibacterial activity against Acinetobacter baumannii DSM 30007 after 18 hrs Acinetobacter baumannii 0.2 ug.mL-1
Antibacterial activity against Klebsiella pneumoniae DSM 11678 after 18 hrs Klebsiella pneumoniae 0.05 ug.mL-1
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum MRC-2 schizont infected in RBC measured after 24 to 30 hrs hrs by giemsa staining based light microscopic method Plasmodium falciparum 50.0 nM
Antimalarial activity against chloroquine-resistant Plasmodium falciparum RKL-9 schizont infected in RBC measured after 24 to 30 hrs hrs by giemsa staining based light microscopic method Plasmodium falciparum 401.0 nM
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay Mus musculus 305.77 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 0.6 ug.mL-1
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining based assay Bacillus subtilis 0.5 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 after 24 hrs by crystal violet staining based assay Staphylococcus aureus 0.4 ug.mL-1
Antibiofilm activity against Micrococcus luteus MTCC 2470 after 24 hrs by crystal violet staining based assay Micrococcus luteus 0.4 ug.mL-1
Antibacterial activity against Staphylococcus aureus ATCC 29213 after 70 to 74 hrs by alamar blue dye based CLSI method Staphylococcus aureus 0.08 ug.mL-1
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 16 to 20 hrs by alamar blue dye based CLSI method Staphylococcus aureus 0.09 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining based method Staphylococcus aureus 700.0 nM
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining based method Bacillus subtilis 600.0 nM
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 after 24 hrs by crystal violet staining based method Staphylococcus aureus 700.0 nM
Antibiofilm activity against Micrococcus luteus MTCC 2470 after 24 hrs by crystal violet staining based method Micrococcus luteus 800.0 nM
Antibiofilm activity against Escherichia coli MTCC 739 after 24 hrs by crystal violet staining based method Escherichia coli 800.0 nM
Antibiofilm activity against Klebsiella planticola MTCC 530 after 24 hrs by crystal violet staining based method Raoultella planticola 600.0 nM
Anti-bacterial activity against Mycobacterium intracellulare ATCC 23068 after 68 to 72 hrs by Alamar blue assay Mycobacterium intracellulare 0.47 ug.mL-1
Anti-bacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by CLSI method Staphylococcus aureus 0.14 ug.mL-1
Anti-bacterial activity against Staphylococcus aureus ATCC 29213 by CLSI method Staphylococcus aureus 0.13 ug.mL-1
Anti-bacterial activity against Escherichia coli ATCC 35218 by CLSI method Escherichia coli 0.007 ug.mL-1
Anti-bacterial activity against Pseudomonas aeruginosa ATCC 27853 by CLSI method Pseudomonas aeruginosa 0.09 ug.mL-1
Inhibition of Escherichia coli N-terminal His6-tagged DNA gyrase subunit GyrA/GyrB supercoiling activity expressed in Escherichia coli BL21 (DE3) using relaxed pBR322 DNA as substrate after 1 hr by agarose gel electrophoresis Escherichia coli 500.0 nM
Inhibition of wild-type Pseudomonas aeruginosa DNA gyrase supercoiling activity using relaxed pBR322 DNA as substrate by ethidium bromide based agarose gel electrophoresis Pseudomonas aeruginosa 500.0 nM
Antibacterial activity against Escherichia coli NCTC 10419 infected in CF mouse assessed as protection against bacterial infection administered orally at 1 and 4 hrs post infection measured after 1 week Escherichia coli 1.25 mg kg-1
Inhibition of Staphylococcus aureus DNA gyrase subunit A supercoiling activity using relaxed pBR322 DNA as substrate after 60 mins by agarose gel electrophoresis Staphylococcus aureus 4.95 ug.mL-1
Inhibition of Staphylococcus aureus DNA gyrase supercoiling activity using pBR322 DNA as substrate after 30 mins by ethidium bromide staining based agarose gel electrophoresis method Staphylococcus aureus 3.5 ug.mL-1
Inhibition of Staphylococcus aureus DNA topoisomerase 4 using Kinetoplast DNA as substrate after 30 mins by ethidium bromide staining based agarose gel electrophoresis method Staphylococcus aureus 1.7 ug.mL-1
Inhibition of Escherichia coli DNA gyrase A2B2 using relaxed pNO1 as substrate Escherichia coli 310.0 nM
Inhibition of His tagged Escherichia coli ATCC 25922 DNA gyrase A expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in enzyme-mediated supercoiling of relaxed plasmid DNA pNO1 after 30 mins in presence of biotinylated TFO1 by fluorescence assay Escherichia coli ATCC 25922 190.0 nM
In vivo antibacterial activity against Escherichia coli NCTC 10419 infected in po dosed mouse administered at 1 and 4 hrs post infection Escherichia coli 1.25 mg kg-1
Antibiofilm activity against Bacillus subtilis MTCC 121 after 24 hrs by crystal violet staining-based assay Bacillus subtilis 0.23 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet staining-based assay Staphylococcus aureus 0.21 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS16 MTCC 2940 after 24 hrs by crystal violet staining-based assay Staphylococcus aureus 0.24 ug.mL-1
Antibiofilm activity against Pseudomonas aeruginosa MTCC 2453 after 24 hrs by crystal violet staining-based assay Pseudomonas aeruginosa 0.32 ug.mL-1
Antibiofilm activity against Klebsiella planticola MTCC 530 after 24 hrs by crystal violet staining-based assay Raoultella planticola 0.29 ug.mL-1
Antimicrobial activity against methicillin-resistant Staphylococcus aureus by modified CLSI based method Staphylococcus aureus 0.12 ug.mL-1
Antimicrobial activity against Staphylococcus aureus by modified CLSI based method Staphylococcus aureus 0.11 ug.mL-1
Inhibition of Escherichia coli DNA gyrase assessed as inhibition of pUC19 supercoiling after 30 mins by agarose gel electrophoresis Escherichia coli 170.0 nM
Inhibition of Escherichia coli DNA topoisomerase-2 mediated DNA relaxation using supercoiled pBR322 plasmid DNA as substrate after 60 mins by ethidium bromide staining based agarose gel electrophoresis Escherichia coli 0.5 ug.mL-1
Inhibition of Escherichia coli DNA topoisomerase-4 mediated decatenation using kinetoplast DNA as substrate after 30 mins agarose gel electrophoresis method Escherichia coli 8.0 ug.mL-1
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging Homo sapiens 2.89 %
Antimicrobial activity against Candida albicans ATCC 90028 assessed as inhibition of microbial growth by CLSI based method Candida albicans 30.0 nM
Antimicrobial activity against Aspergillus fumigatus ATCC 90906 assessed as inhibition of microbial growth by CLSI based method Aspergillus fumigatus 30.0 nM
Antimicrobial activity against Cryptococcus neoformans ATCC 90113 assessed as inhibition of microbial growth by CLSI based method Cryptococcus neoformans 30.0 nM
Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of microbial growth by CLSI based method Staphylococcus aureus 30.0 nM
Antimicrobial activity against Escherichia coli ATCC 35218 assessed as inhibition of microbial growth by CLSI based method Escherichia coli 0.03 nM
Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 assessed as inhibition of microbial growth by CLSI based method Pseudomonas aeruginosa 0.3 nM
Antibacterial activity against Klebsiella pneumoniae ATCC 13883 incubated for 24 hrs by resazurin dye based fluorimetric assay Klebsiella pneumoniae 250.0 nM
Inhibition of Escherichia coli DNA gyrase super-coiling activity using relaxed pNO1 DNA as substrate incubated for 30 mins by fluorescence assay Escherichia coli 122.0 nM
Antibacterial activity against Escherichia coli K-12 BW25113 incubated for 18 hrs by broth microdilution method Escherichia coli 22.0 nM
Antibacterial activity against Staphylococcus aureus SH1000 incubated for 18 hrs by broth microdilution method Staphylococcus aureus 350.0 nM
Inhibition of Escherichia coli DNA gyrase (A2B2 tetramer) using relaxed pBR322 as substrate preincubated for 30 mins followed by enzyme addition by SYBR staining-based agarose gel electrophoresis method Escherichia coli 280.0 nM
Antibiofilm activity against Bacillus subtilis MTCC 121 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Bacillus subtilis 6.6 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MLS-16 MTCC 2940 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Staphylococcus aureus 6.6 ug.mL-1
Antibiofilm activity against Micrococcus luteus MTCC 2470 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Micrococcus luteus 6.8 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Staphylococcus aureus 6.7 ug.mL-1
Antibiofilm activity against Escherichia coli MTCC 739 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Escherichia coli 7.3 ug.mL-1
Antibiofilm activity against Pseudomonas aeruginosa MTCC 2453 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Pseudomonas aeruginosa 7.4 ug.mL-1
Antibiofilm activity against Klebsiella planticola MTCC 530 assessed as inhibition of biofilm formation by crystal violet staining-based microtitre plate assay Raoultella planticola 8.6 ug.mL-1
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Homo sapiens 53.4 ug.mL-1
Antibiofilm activity against Escherichia coli MTCC 739 assessed as inhibition of biofilm formation incubated for 48 hrs in presence of Staphylococcus aureus MTCC 96 by FE-SEM analysis Escherichia coli 11.6 ug.mL-1
Antibiofilm activity against Staphylococcus aureus MTCC 96 assessed as inhibition of biofilm formation incubated for 48 hrs in presence of Escherichia coli MTCC 739 by FE-SEM analysis Staphylococcus aureus 11.6 ug.mL-1
Antibiofilm activity against ofloxacin-resistant Bacillus megaterium assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Bacillus megaterium 56.3 %
Antibiofilm activity against tetracycline-resistant Bacillus subtilis assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Bacillus subtilis 23.0 %
Antibiofilm activity against carbapenem-resistant Escherichia coli assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Escherichia coli 45.0 %
Antibiofilm activity against tetracycline-resistant Pseudomonas fluorescens assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Pseudomonas fluorescens 38.0 %
Antibiofilm activity against carbenicillin-resistant Pseudomonas aeruginosa assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Pseudomonas aeruginosa 49.7 %
Antibiofilm activity against carbapenem-resistant Klebsiella pneumoniae assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Klebsiella pneumoniae 25.5 %
Antibiofilm activity against tetracycline-resistant Klebsiella pneumoniae assessed as disruption of biofilm at 200 ug/ml after 24 hrs by crystal violet staining based ELISA relative to control Klebsiella pneumoniae 43.0 %
Inhibition of Escherichia coli JMtacA/JMtacB DNA gyrase subunit A2B2 S83W mutant using relaxed pBR322 DNA as substrate incubated for 30 mins in presence of ATP by ethidium bromide staining based agarose gel electrophoresis Escherichia coli 500.0 nM
Cytotoxicity against human HepG2 cells after 24 hrs by cell titre-glo assay Homo sapiens 128.0 ug.mL-1
Inhibition of human ERG channel at 100 uM by automated patch clamp assay Homo sapiens 28.0 %
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate Severe acute respiratory syndrome coronavirus 2 16.68 % SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate Severe acute respiratory syndrome coronavirus 2 13.11 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.08 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.14 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.08 % Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Chlorocebus sabaeus 0.14 %
Inhibition of Staphylococcus aureus DNA gyrase using relaxed pNO1 as substrate by gel based fluorescence assay Staphylococcus aureus 13.05 ug.mL-1
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Homo sapiens 302.0 nM
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Homo sapiens 302.0 nM
Inhibition of recombinant full-length C-terminal His6-tagged Escherichia coli DNA gyrase AB supercoiling activity using relaxed DNA as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs in presence of ATP by size exclusion HPLC analysis Escherichia coli 490.0 nM
Inhibition of Escherichia coli DNA gyrase using relaxed PBR322 plasmid DNA as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis method Escherichia coli 200.0 nM
Inhibition of biofilm formation in Pseudomonas aeruginosa MTCC 2453 incubated for 24 hrs by crystal violet staining based microtiter plate method Pseudomonas aeruginosa 500.0 nM
Inhibition of biofilm formation in Escherichia coli MTCC 739 incubated for 24 hrs by crystal violet staining based microtiter plate method Escherichia coli 600.0 nM
Inhibition of biofilm formation in Klebsiella planticola MTCC 530 incubated for 24 hrs by crystal violet staining based microtiter plate method Raoultella planticola 800.0 nM
Inhibition of biofilm formation in Micrococcus luteus MTCC 2470 incubated for 24 hrs by crystal violet staining based microtiter plate method Micrococcus luteus 800.0 nM
Inhibition of biofilm formation in Bacillus subtilis MTCC 121 incubated for 24 hrs by crystal violet staining based microtiter plate method Bacillus subtilis 700.0 nM
Inhibition of biofilm formation in Staphylococcus aureus MLS16 MTCC 2940 incubated for 24 hrs by crystal violet staining based microtiter plate method Staphylococcus aureus 700.0 nM
Inhibition of biofilm formation in Staphylococcus aureus MTCC 92 incubated for 24 hrs by crystal violet staining based microtiter plate method Staphylococcus aureus 600.0 nM
Inhibition of Escherichia coli DNA gyrase using relaxed DNA as substrate incubated for 15 mins by ethidium bromide-based agarose gel electrophoresis Escherichia coli 440.0 nM
Antibacterial activity against Salmonella enterica MTCC 3224 incubated overnight by broth dilution technique Salmonella enterica 0.012 ug.mL-1
Antibacterial activity against Pseudomonas aeruginosa MTCC 2453 incubated overnight by broth dilution technique Pseudomonas aeruginosa 0.012 ug.mL-1
Antibacterial activity against Enterococcus faecalis MTCC 439 incubated overnight by broth dilution technique Enterococcus faecalis 0.012 ug.mL-1
Antibacterial activity against Streptococcus pneumoniae MTCC 655 incubated overnight by broth dilution technique Streptococcus pneumoniae 0.012 ug.mL-1
Antibacterial activity against Klebsiella pneumoniae ATCC 700603 incubated overnight by broth dilution technique Klebsiella pneumoniae 0.012 ug.mL-1
Antibacterial activity against Escherichia coli ATCC 25922 incubated overnight by broth dilution technique Escherichia coli 0.012 ug.mL-1
Inhibition of DNA synthesis in Staphylococcus aureus ATCC 29213 at 8 times MIC measured by liquid scintillation counter Staphylococcus aureus 86.2 %
Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of bacterial growth by CLSI method Staphylococcus aureus 0.09 ug.mL-1
Antibacterial activity against vancomycin resistant Enterococcus ATCC MP-1 assessed as inhibition of bacterial growth by CLSI method Enterococcus 0.15 ug.mL-1
Antibacterial activity against Escherichia coli ATCC 35218 assessed as inhibition of bacterial growth by CLSI method Escherichia coli 0.007 ug.mL-1
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as inhibition of bacterial growth by CLSI method Pseudomonas aeruginosa 0.09 ug.mL-1
Inhibition of Staphylococcus aureus topoisomerase 4 assessed as reduction in decatenation using kDNA as substrate incubated for 30 mins by fluorimetric assay Staphylococcus aureus 550.0 nM
Inhibition of Escherichia coli DNA gyrase supercoiling activity using pBR322 as substrate incubated for 30 mins by fluorimetric assay Escherichia coli 830.0 nM

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Cross References

Resources Reference
ChEBI 100241
ChEMBL CHEMBL8
DrugBank DB00537
DrugCentral 659
FDA SRS 5E8K9I0O4U
Human Metabolome Database HMDB0014677
Guide to Pharmacology 10902
KEGG C05349
PDB CPF
PharmGKB PA449009
PubChem 2764
SureChEMBL SCHEMBL2900
ZINC ZINC000000020220