Syntheses of novel antimycobacterial combinatorial libraries of structurally diverse substituted pyrimidines by three-component solid-phase reactions.
作者： Arun Kumar , Sudhir Sinha , Prem M.S Chauhan
DOI: 10.1016/S0960-894X(01)00829-0
关键词: Antimycobacterial 、 Stereochemistry 、 Chemical synthesis 、 Nitrile 、 Antibacterial agent 、 Structure–activity relationship 、 Chemistry 、 Combinatorial Chemistry Techniques 、 Mycobacterium tuberculosis 、 Pyrimidine
摘要: A new pyrimidine based scaffold has been developed by three-component solid-phase syntheses. The utility of scaffolds was demonstrated by synthesizing libraries of 80 substituted pyrimidines 12 (a–p), 13 (a–p), 14 (a–p), 15 (a–p), 16 (a–p). Among 80 compounds screened, six compounds, 12i, 13c, 14d, 14e, 14o, and 15d showed in vitro activity against Mycobacterium tuberculosis (MABA) at a concentration of 50 and 25 μg/mL
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