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

L Ballell, RA Field, GAC Chung, RJ Young

文献索引：Ballell, Lluis; Field, Robert A.; Chung, Gavin A.C.; Young, Robert J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1736 - 1740

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被引用次数: 76

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⩽ 2μg/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.