New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents

被引：101

作者：

Ballell, Lluis ^{[1
]}

Field, Robert A.

Chung, Gavin A. C.

Young, Robert J.

机构：

[1] Univ E Anglia, Sch Chem Sci & Pharm, Ctr Carbohydrate Chem, Norwich NR4 7TJ, Norfolk, England

[2] GlaxoSmithKline, Med Res Ctr, Stevenage SG1 2NY, Herts, England

[3] GlaxoSmithKline, MMPD CEDD, DDW, Tres Cantos 28760, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 06期

基金：

英国生物技术与生命科学研究理事会;

关键词：

anti-mycobacterial; anti-tubercular; thiopyrazolopyrimidines; SAR; SULFOTRANSFERASE INHIBITORS; DISCOVERY; TUBERCULOSIS; DESIGN;

D O I：

10.1016/j.bmcl.2006.12.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to < 2 mu/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1736 / 1740

页数：5

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