Potent DNA gyrase inhibitors; novel 5-vinylpyrazole analogues with Gram-positive antibacterial activity

被引：35

作者：

Tanitame, A

Oyamada, Y

Ofuji, K

Suzuki, K

Ito, H

Kawasaki, M

Wachi, M

Yamagishi, J

机构：

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

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

[3] Tokyo Inst Technol, Dept Bioengn, Midori Ku, Yokohama, Kanagawa 2268501, Japan

来源：

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

关键词：

DNA gyrase inhibitor; 5-Vinylpyrazole analogues; multidrug resistant strains;

D O I：

10.1016/j.bmcl.2004.03.045

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 designed and synthesized novel 5-vinylpyrazole analogues by decreasing the lipophilicity of the parent compounds 1a,b; 3-[(3-methoxycarbonyl)cyclohexylaminomethyl]indazoles while keeping the van der Waals interaction with the lipophilic area of DNA gyrase B. The selected compound 8bb exhibited good antibacterial activity against staphylococci and enterococci, including multi-drug resistant strains. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2863 / 2866

页数：4

共 12 条

[1]

*BIOB CORP, CLOPS THES COMP CALC

[2]

MANNICH-BASES OF 4-PHENYL-3-BUTEN-2-ONE - A NEW CLASS OF ANTIHERPES AGENT [J].