Novel dihydropyrimidines as a potential new class of antitubercular agents

作者：Trivedi Amit R; Bhuva Vimal R; Dholariya Bipin H; Dodiya Dipti K; Kataria Vipul B; Shah Viresh H^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(20): 6100-6102.

DOI：10.1016/j.bmcl.2010.08.046

• Dihydropyrimidines
• Antitubercular activity
• Antimycobacterial activity
• Mycobacterium tuberculosis H(37)Rv
• DHFR (dihydrofolate reductase)

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 mu g/mL against MTB and were more potent than isoniazid.

• 出版日期2010-10-15