title: Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.
abstract: In this study, we report the design, synthesis and structure-activity relationships of novel indazole derivatives as DNA gyrase inhibitors with Gram-positive antibacterial activity. Our results show that selected compounds from this series exhibit potent antibacterial activity against Gram-positive bacteria including multi-drug resistant strains that is methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE).
authors.affiliation: Chemistry 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: Yoko
authors.initials: Y
authors.lastname: Kyoya
authors.forename: Kenji
authors.initials: K
authors.lastname: Suzuki
authors.forename: Hideaki
authors.initials: H
authors.lastname: Ito
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* / Q000494:pharmacology; D026942:DNA Topoisomerases / Q000187:drug effects; D015195:Drug Design; D018432:Drug Resistance, Multiple; D013293:Enterococcus faecalis / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D040141:Staphylococcaceae / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D059005:Topoisomerase II Inhibitors; D026942:DNA Topoisomerases