α-substituted hydroxamic acids as novel bacterial deformylase inhibitor-based antibacterial agents

被引：29

作者：

Jain, R

Sundram, A

Lopez, S

Neckermann, G

Wu, C

Hackbarth, C

Chen, D

Wang, W

Ryder, NS

Weidmann, B

Patel, D

Trias, J

White, R

Yuan, Z

机构：

[1] Vicuron Pharmaceut, Fremont, CA 94555 USA

[2] Novartis Inst Biomed Res Inc, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2003.07.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and biological activity of analogues of VRC3375 (N-hydroxy-3-R-butyl-3-[(2-S-(tert-butoxycarbonyl)-pyrrolidin-1-ylcarbonyl]propionamide), an orally active peptide deformylase inhibitor. This study explores the structureactivity relationship of various chelator groups, alpha substituents, P-2' and P-3' substituents in order to achieve optimal antibacterial activity with minimal toxicity liability. (C) 2003 Elsevier Ltd. All rights reserved.

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收藏

页码：4223 / 4228

页数：6

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