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

Ballell, Lluis, Field, Robert A. ORCID: https://orcid.org/0000-0001-8574-0275, Chung, Gavin A. C. and Young, Robert J. (2007) New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents. Bioorganic and Medicinal Chemistry Letters, 17 (6). pp. 1736-1740. ISSN 0960-894X

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Abstract

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.

Item Type:	Article
Additional Information:	Funding Information: We thank the GlaxoSmithKline Action TB Initiative for financial support and María Jesús Almela for generating the cytotoxicity data.
Uncontrolled Keywords:	anti-mycobacterial,anti-tubercular,sar,thiopyrazolopyrimidines,biochemistry,molecular medicine,molecular biology,pharmaceutical science,drug discovery,clinical biochemistry,organic chemistry ,/dk/atira/pure/subjectarea/asjc/1300/1303
Faculty \ School:	Faculty of Science > School of Chemical Sciences and Pharmacy (former - to 2009)
Related URLs:	http://www.scopus.com/inward/record.url?...
Depositing User:	LivePure Connector
Date Deposited:	06 Sep 2024 13:35
Last Modified:	25 Sep 2024 18:07
URI:	https://ueaeprints.uea.ac.uk/id/eprint/96612
DOI:	10.1016/j.bmcl.2006.12.066

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