title: Synthesis and antibacterial activity of a novel series of potent DNA gyrase inhibitors. Pyrazole derivatives.
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.
authors.affiliation: Chemistry Research Laboratories, Pharmacology and Microbiology Research Laboratories, Dainippon Pharmaceutical Co. Ltd., 33-94 Enoki, Suita, Osaka 564-0053, Japan. akihiko-tanitame@dainippon-pharm.co.jp
authors.forename: Akihiko
authors.initials: A
authors.lastname: Tanitame
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Oyamada
authors.forename: Keiko
authors.initials: K
authors.lastname: Ofuji
authors.forename: Mika
authors.initials: M
authors.lastname: Fujimoto
authors.forename: Noritaka
authors.initials: N
authors.lastname: Iwai
authors.forename: Yoichi
authors.initials: Y
authors.lastname: Hiyama
authors.forename: Kenji
authors.initials: K
authors.lastname: Suzuki
authors.forename: Hideaki
authors.initials: H
authors.lastname: Ito
authors.forename: Hideo
authors.initials: H
authors.lastname: Terauchi
authors.forename: Motoji
authors.initials: M
authors.lastname: Kawasaki
authors.forename: Kazuo
authors.initials: K
authors.lastname: Nagai
authors.forename: Masaaki
authors.initials: M
authors.lastname: Wachi
authors.forename: Jun-ichi
authors.initials: J
authors.lastname: Yamagishi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D024881:Drug Resistance, Bacterial; D013293:Enterococcus faecalis / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: C488120:5-(2-(5-chloroindol-3-yl)vinyl)pyrazole; D000900:Anti-Bacterial Agents; D007211:Indoles; D011720:Pyrazoles; D059005:Topoisomerase II Inhibitors; D027101:DNA Topoisomerase IV