Bioorganic & Medicinal Chemistry Letters 2004-06-07

Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.

Akihiko Tanitame, Yoshihiro Oyamada, Keiko Ofuji, Yoko Kyoya, Kenji Suzuki, Hideaki Ito, Motoji Kawasaki, Kazuo Nagai, Masaaki Wachi, Jun-ichi Yamagishi

Index: Bioorg. Med. Chem. Lett. 14 , 2857-2862, (2004)

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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).