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Novel dihydropyrimidines as a potential new class of antitubercular agents

2010; Elsevier BV; Volume: 20; Issue: 20 Linguagem: Inglês

10.1016/j.bmcl.2010.08.046

1464-3405

Amit R. Trivedi, Vimal R. Bhuva, Bipin H. Dholariya, Dipti K. Dodiya, Vipul B. Kataria, Viresh H. Shah,

Synthesis and biological activity

A small library of 30 dihydropyrimidines was synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. Two compounds, ethyl 4-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxylate 4a and ethyl 4-[3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate 4d were found to be the most active compounds in vitro with MIC of 0.02 μg/mL against MTB and were more potent than isoniazid.