Synthesis and Antibacterial Activity of a Novel Series of Potent DNA Gyrase Inhibitors. Pyrazole Derivatives
Journal of Medicinal Chemistry2004Vol. 47(14), pp. 3693–3696
Citations Over TimeTop 10% of 2004 papers
Akihiko Tanitame, Yoshihiro Oyamada, Keiko Ofuji, Mika Fujimoto, Noritaka Iwai, Yoichi Hiyama, Kenji Suzuki, Hideaki Ito, Hideo Terauchi, Motoji Kawasaki, Kazuo Nagai, Masaaki Wachi, Jun‐ichi Yamagishi
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.
Related Papers
- → Comparison of inhibition of Escherichia coli topoisomerase IV by quinolones with DNA gyrase inhibition(1994)162 cited
- → Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria(2020)36 cited
- → Conjugation between quinolone-susceptible bacteria can generate mutations in the quinolone resistance-determining region, inducing quinolone resistance(2014)13 cited
- → DNA Topoisomerases from Streptomyces and Their Inhibition by Some Antibiotic and Antitumoractive Agents(1991)1 cited
- → Non-Quinolone Inhibitors of the Bacterial DNA Gyrase(2021)