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


Synthesis and Antimicrobial Evaluation of Some New Dihydropyrimidine Derivatives

Author(s): Ashraf M. Hamouda and Khaled O. Mohamed

By the application of Beginili conditions, a new series of 1-substituted and 1-unsubstituted of 5-cyano-2-thiouracil 1(a-h) derivatives were synthesized and evaluated for their antimicrobial activities. Reacting our main tautomeric target compound 6-(benzo[b]thiophen-2-yl)-4-oxo-2-thioxo-1,2,3,4- tetrahydropyrimidine -5-carbonitrile (1a) with methyl iodide gave the dimethyl derivative 2 . Hydrazinolysis of compound 2 yielded the hydrazino compound 3, which was converted to the corresponding pyrazole derivatives 4 (a,b) by reacting with1-(4-bromophenyl)-3-(4- bromo or 4-fluorophenyl) prop-2-en-1-one. A series of azomethine compounds 6 (a-d) were obtained by reacting the hydrazino compound 5 with different aromatic aldehydes, which was obtained by hydrazinolysis of compound 1a with hydrazine hydrate. All the compounds were characterized by physical and spectral data. The compounds were screened for anti-microbial activity