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

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

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          Author and article information

          Journal
          Bioorg. Med. Chem. Lett.
          Bioorganic & medicinal chemistry letters
          Elsevier BV
          0960-894X
          0960-894X
          Mar 15 2007
          : 17
          : 6
          Affiliations
          [1 ] Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK. lluis.p.ballell@gsk.com
          Article
          S0960-894X(06)01469-7
          10.1016/j.bmcl.2006.12.066
          17239593
          b0f40354-ef2f-43b6-bcc2-093f531f11e0
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