Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 6, Pages 1736-1740Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.066
Keywords
anti-mycobacterial; anti-tubercular; thiopyrazolopyrimidines; SAR
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Funding
- Biotechnology and Biological Sciences Research Council [BBS/E/J/000C0618] Funding Source: Medline
- BBSRC [BBS/E/J/000C0618] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BBS/E/J/000C0618] Funding Source: researchfish
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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.
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