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

被引:98
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
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
收藏
页码:1736 / 1740
页数:5
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