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

页码：5668 / 5672

页数：5

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