Synthesis and Antibacterial Activity of a Novel Series of Potent DNA Gyrase Inhibitors. Pyrazole Derivatives
Top Cited Papers
- 5 June 2004
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (14), 3693-3696
- https://doi.org/10.1021/jm030394f
Abstract
We have previously found that a pyrazole derivative 1 possesses antibacterial activity and inhibitory activity against DNA gyrase and topoisomerase IV. Here, we synthesized new pyrazole derivatives and found that 5-[(E)-2-(5-chloroindol-3-yl)vinyl]pyrazole 16 possesses potent antibacterial activity and selective inhibitory activity against bacterial topoisomerases. Many of the synthesized pyrazole derivatives were potent against clinically isolated quinolone- or coumarin-resistant Gram-positive strains and had minimal inhibitory concentration values against these strains equivalent to those against susceptible strains.This publication has 7 references indexed in Scilit:
- Novel Inhibitors of DNA Gyrase: 3D Structure Based Biased Needle Screening, Hit Validation by Biophysical Methods, and 3D Guided Optimization. A Promising Alternative to Random ScreeningJournal of Medicinal Chemistry, 2000
- Irregular nuclear localization and anucleate cell production in Escherichia coli induced by a Ca2+ chelator, EGTABiochimie, 1999
- GyrB mutations in Staphylococcus aureus strains resistant to cyclothialidine, coumermycin, and novobiocinAntimicrobial Agents and Chemotherapy, 1996
- 5-(4-Chlorophenyl)-4-methyl-3-(1-(2- phenylethyl)piperidin-4-yl)isoxazole: A Potent, Selective Antagonist at Human Cloned Dopamine D4 ReceptorsJournal of Medicinal Chemistry, 1996
- Cloning and primary structure of Staphylococcus aureus DNA topoisomerase IV: a primary target of fluoroquinolonesMolecular Microbiology, 1994
- The interaction between coumarin drugs and DNA gyraseMolecular Microbiology, 1993
- Pyridonecarboxylic acids as antibacterial agents. Part 14. Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potencyJournal of Medicinal Chemistry, 1990