Synthesis of sub-micromolar inhibitors of MraY by exploring the region originally occupied by the diazepanone ring in the liposidomycin structure

被引：47

作者：

Dini, C ^{[1
]}

Didier-Laurent, S ^{[1
]}

Drochon, N ^{[1
]}

Feteanu, S ^{[1
]}

Guillot, JC ^{[1
]}

Monti, F ^{[1
]}

Uridat, E ^{[1
]}

Zhang, J ^{[1
]}

Aszodi, J ^{[1
]}

机构：

[1] Aventis Pharma, Paris Res Ctr, F-93235 Romainville, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(02)00109-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and inhibitory activity against MraY of a series of simplified analogues of liposidomycins are described. These compounds were mainly obtained by performing parallel synthesis in the 6'-position of a scaffold that gathers key features found necessary for the binding to MraY. Thus, inhibitory activity was improved from 5300 to 140 nM. This improvement was correlated with the length and lipophilicity of substituents, but was found to be independent of the nature of the chemical bond generated. In addition, some of these inhibitors presented encouraging antibacterial activities. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1209 / 1213

页数：5

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