Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.
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).
Tanitame
Akihiko
A
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, 33-94, Enoki, Suita, Osaka 564-0053, Japan. akihiko-tanitame@dainippon-pharm.co.jp
Oyamada
Yoshihiro
Y
Ofuji
Keiko
K
Kyoya
Yoko
Y
Suzuki
Kenji
K
Ito
Hideaki
H
Kawasaki
Motoji
M
Nagai
Kazuo
K
Wachi
Masaaki
M
Yamagishi
Jun-ichi
J
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
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D059005:Topoisomerase II Inhibitors; D026942:DNA Topoisomerases