Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones

被引：40
作者：
Boros, Eric E. [1 ]
Johns, Brian A. [1 ]
Garvey, Edward P. [1 ]
Koble, Cecilia S. [1 ]
Miller, Wayne H. [1 ]
机构：
[1] GlaxoSmithKline Res & Dev Ltd, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 21期
关键词：
HIV-integrase; strand-transfer inhibition;
D O I：
10.1016/j.bmcl.2006.08.007
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
An efficient synthesis of methyl 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-one-6-carboxylates (8-10 and 16) and 6-carboxamides (17-20) is described. Sub-micromolar enzyme inhibition of HIV integrase was achieved with several carboxamide analogs which were superior to their carboxylic ester congeners. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5668 / 5672
页数：5
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