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

被引：71

作者：

Tanitame, A

Oyamada, Y

Ofuji, K

Kyoya, Y

Suzuki, K

Ito, H

Kawasaki, M

Nagai, K

Wachi, M

Yamagishi, J

机构：

[1] Dainippon Pharmaceut Co Ltd, Chem Res Labs, Osaka 5640053, Japan

[2] Dainippon Pharmaceut Co Ltd, Pharmacol & Microbiol Res Labs, Suita, Osaka 5640053, Japan

[3] Chubu Univ, Dept Biol Chem, Kasugai, Aichi 4878501, Japan

[4] Tokyo Inst Technol, Dept Bioengn, Midori Ku, Yokohama, Kanagawa 4878501, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

关键词：

DNA gyrase inhibitor; Indazole analogues; multi-drug resistant strains; ATP binding site;

D O I：

10.1016/j.bmcl.2004.03.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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). (C) 2004 Elsevier Ltd. All rights reserved.

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页码：2857 / 2862

页数：6

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