Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines |
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Authors: | Matthew L Read Morten Brændvang Pedro O Miranda Lise-Lotte Gundersen |
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Institution: | Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N-0315 Oslo, Norway;Max-Planck-Institute for Molecular Physiology, Dept of Chemical Biology, Otta-Hahn-Strasse 11, 44227 Dortmund, Germany |
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Abstract: | Pyrimidine analogs of antimycobacterial 6-aryl-9-benzylpurines have been synthesized and screened for antibacterial activity against Mycobacterium tuberculosis H37Rv in vitro. Several active compounds were identified and the best results were observed for 5-formamidopyrimidines. These compounds generally displayed IC90 values ≤1 μg/mL, and they exhibited low toxicity towards mammalian cells. Imidazolylpyrimidines, which may be regarded as fleximer analogs of the parent purines, were also synthesized and one of them was found to be quite a potent inhibitor of M. tuberculosis (IC90 14 μg/mL). |
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