Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines |
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Institution: | 1. Department of Chemistry, Kakatiya University, Warangal 506009, India;2. Department of Chemistry, Kakatiya Institute of Technology and Science, Warangal 506015, India |
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Abstract: | Various 5-(fluoroaryl)-4-(hetero)aryl substituted pyrimidines have been synthesized based on the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (SNH) reactions starting from commercially available 5-bromopyrimidine and their antitubercular activity against Mycobacterium tuberculosis H37Rv has been explored. The outcome of the study disclose that, some of the compounds have showed promising activity in micromolar concentration against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant strains isolated from tuberculosis patients in Ural region (Russia). The data concerning the ‘structure–activity’ relationship for fluorinated compounds have been discussed. |
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Keywords: | Pyrimidine Antimycobacterial Tuberculosis Cross-coupling Nucleophilic aromatic substitution of hydrogen |
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