Synthesis, spectral investigation and biological evaluation of novel hydrazones derivative of substituted 1,2-dihydropyrimidine ring

In this study, 6-methyl-2-oxo-4-phenyl-1,2-dihydropyrimidine-5-carbohydrazide (2) was synthesized by facile and fast procedure using ethyl 6-methyl-2-oxo-4-phenyl-1,2-dihydropyrimidine-5-carboxylate (1) with hydrazine, which further underwent condensation with various aromatic aldehydes to afford N'-benzylidene-6-methyl-2-oxo-4-phenyl- 1,2-dihydro pyrimidine-5-carbohydrazide (3a-h). Compounds (3a-h) were used as precursor for the preparation of various 6-methyl-2-oxo-N-(4-oxo-2-phenylthiazolidin-3-yl)-4-phenyl-1,2-dihydro pyrimidine-5-carboxamide (4a-h). All synthesized compounds were characterized by various spectroscopic techniques and screened for their in-vitro antimicrobial activity. Also MIC (Minimum inhibitory concentration) values of these compounds were determined. The investigation of antimicrobial screening data revealed that most of the compounds tested have demonstrated congruent activity. In summary, preliminary results indicate that, the compounds 3g, 3f, 4g and 4f found to possess better antibacterial activity than Tetracycline (Reference standard) in MIC also compounds 3g ,4e.4f and 4g found to possess better antifungal activity against Trichphyton longifusus and Candida glabrata than Miconazole (Reference standard).

Author(s): Haitham Al-Sharifi and Hasmukh S. Patel

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