Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis and antimicrobial activity of some ethyl [6-methyl-2-methoxy-3-(substituted phenylethanone)-4-(substituted phenyl)]-1,2,3,4-tetrahydropyrimidine-5-carboxylates

Author(s): R. V. Chikhale, R. P. Bhole, P. A. Patil, P. B. Khedekar, K. P. Bhusari

Fifteen new ethyl 6-methyl-2-methoxy-3-(substituted 1-phenylethanone)-4-(Substituted phenyl)- 1,2,3,4-tetrahydropyrimidine-5-carboxylates (6.a-o) have been synthesized in a two step reaction. In first step ethyl acetoacetate, s-methylisourea and appropriate benzaldehydes reacted in a single step reaction to obtain ethyl 6-methyl-2-methoxy-4-(substituted phenyl) -1, 4- dihydropyrimidine-5-carboxylates (4.a-e). Second step involves synthesis of reaction between substituted phenacyl bromides and 1-4 dihydropyrimidine-5-carboxylates (6.a-o). Their structures are confirmed by IR, 1H- NMR, Mass and elemental analysis. Out of the total screened compounds, 6 compounds have shown antitubercular activity against Mycobacterium tuberculosis H37Rv in concentration range of 1-2 μg/mL. Eight compounds have shown good activity against gram positive (S. aureus and B. subtilis) and gram negative organisms (E. coli and S. typhi), ranging in the concentration from 1-25 μg/mL.


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