Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease

被引：51
|
作者：
Dhanak, D
Keenan, RM
Burton, G
Kaura, A
Darcy, MG
Shah, DH
Ridgers, LH
Breen, A
Lavery, P
Tew, DG
West, A
机构：
[1] SmithKline Beecham Pharmaceut, Collegeville, PA 19426 USA
[2] SmithKline Beecham Pharmaceut, Harlow CM19 5AG, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期
关键词：
D O I：
10.1016/S0960-894X(98)00666-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel class of CMV protease inhibitors based on a benzothiopyran-S,S-dioxide nucleus has been discovered. Enzyme kinetic data supports a reversible mode of inhibition for a representative member of this class, 2-(3-pyridyl-N-oxide)benzothiopyran-4-one-S,S-dioxide, 1. Experiments in the presence and absence of the disulfide reducing agent DTT suggest that the inhibition by 1 is not due to oxidative inactivation of the enzyme. Also presented are results of some SAR studies of the benzothiopyranone ring system. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：3677 / 3682
页数：6
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