DNA binding ligands targeting drug-resistant Gram-positive bacteria.: Part 2:: C-terminal benzimidazoles and derivatives

被引：63

作者：

Bürli, RW ^{[1
]}

Jones, P ^{[1
]}

McMinn, D ^{[1
]}

Le, Q ^{[1
]}

Duan, JX ^{[1
]}

Kaizerman, JA ^{[1
]}

Difuntorum, S ^{[1
]}

Moser, HE ^{[1
]}

机构：

[1] Genesoft Pharmaceut Inc, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 05期

关键词：

antibiotics; DNA binder; minor groove; lead optimization;

D O I：

10.1016/j.bmcl.2003.12.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and in vitro potency of DNA minor-groove binding antibacterials lacking the C-terminal amide bond are described. The crescent shaped molecules bear the positively charged amino group at an internal pyrrole unit instead of the C-terminus. Three structural parameters were investigated: the N-terminal unit, the internal amino group, and the C-terminal ring system. Several compounds demonstrated good in vitro potency against various Gram-positive bacteria and some molecules were moderately active against Escherichia coli, a representative Gram-negative strain. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：1259 / 1263

页数：5

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