Design and synthesis of monocyclic β-lactams as mechanism-based inhibitors of human cytomegalovirus protease.

被引：174

作者：

Borthwick, AD

Weingarten, G

Haley, TM

Tomaszewski, M

Wang, W

Hu, ZH

Bedard, J

Jin, HL

Yuen, L

Mansour, TS

机构：

[1] Glaxo Wellcome Res & Dev Ltd, Med Res Ctr, Dept Enzyme Med Chem 2, Stevenage SG1 2NY, Herts, England

[2] Dept Med Chem & Virol, Quebec City, PQ H7V 4A7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(98)00032-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependant manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined the size and relative stereochemisty of the C-3 substituent producing a low micromolar inhibitor 17b with good aqueous stability and selectivity over the mammalian serine proteases. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：365 / 370

页数：6

共 12 条

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