799279-19-9Relevant articles and documents
Synthesis and antibacterial activity of novel and potent DNA gyrase inhibitors with azole ring
Tanitame, Akihiko,Oyamada, Yoshihiro,Ofuji, Keiko,Fujimoto, Mika,Suzuki, Kenji,Ueda, Tomohiko,Terauchi, Hideo,Kawasaki, Motoji,Nagai, Kazuo,Wachi, Masaaki,Yamagishi, Jun-Ichi
, p. 5515 - 5524 (2007/10/03)
The pyrazole, oxazole and imidazole derivatives synthesized in this study exhibited potent antibacterial activity against multidrug resistant Gram-positive bacteria with minimal inhibitory concentration values equivalent to those against susceptible strains. The 4-piperidyl moiety and the pyrazole ring in 1-(3-chlorophenyl)-5-(4-phenoxyphenyl)-3-(4-piperidyl)pyrazole 2, which has previously shown improved DNA gyrase inhibition and target-related antibacterial activity, were transformed to other groups and the in vitro antibacterial activity of the synthesized compounds was evaluated. The selected pyrazole, oxazole and imidazole derivatives showed moderate inhibition against DNA gyrase and topoisomerase IV with similar IC50 values (IC 50 = 9.4-25 μg/mL). In addition, many of the pyrazole, oxazole a1nd imidazole derivatives synthesized in this study exhibited potent antibacterial activity against quinolone-resistant clinical isolates and coumarin-resistant laboratory isolates of Gram-positive bacteria with minimal inhibitory concentration values equivalent to those against susceptible strains.