- Novel dihydropyrimidines as a potential new class of antitubercular agents.
Novel dihydropyrimidines as a potential new class of antitubercular agents.
Bioorganic & medicinal chemistry letters (2010-09-04)
Amit R Trivedi, Vimal R Bhuva, Bipin H Dholariya, Dipti K Dodiya, Vipul B Kataria, Viresh H Shah
PMID20813528
摘要
A small library of 30 dihydropyrimidines was synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H(37)Rv. 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.
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