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

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

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