Novel dihydropyrimidines as a potential new class of antitubercular agents

A small library of 30 dihydropyrimidines was synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H 37Rv. Two compounds, ethyl 4-[3-(4-fluorophenyl)-1-phenyl-1 H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxylate 4a and ethyl 4-...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-10, Vol.20 (20), p.6100-6102
Hauptverfasser: Trivedi, Amit R., Bhuva, Vimal R., Dholariya, Bipin H., Dodiya, Dipti K., Kataria, Vipul B., Shah, Viresh H.
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Sprache:eng
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Zusammenfassung:A small library of 30 dihydropyrimidines was synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H 37Rv. Two compounds, ethyl 4-[3-(4-fluorophenyl)-1-phenyl-1 H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxylate 4a and ethyl 4-[3-(4-nitrophenyl)-1-phenyl-1 H-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.08.046