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New potential chemotherapeutic strategies are required to overcome multidrug resistance (MDR) in cancer. In this study, Antibacterial activities of the synthesized compounds were evaluated against gram (+) Staphylococcus aureus and gram (-) Klebsilla aerogenes by measuring zone of inhibition. The antifungal activities of the synthesized compounds were evaluated against Candida albicans by disc diffusion method. Compounds screened for antibacterial activity against Bacillus subtilis, Escherichia coli. and antifungal activity against Candida albicans, Aspergillus Niger by cup plate method. All the compounds of the series were screened for their antibacterial and antifungal activity studies. Substitution of hydroxyl and halo groups emerged as active in both antibacterial and antifungal screening. The reported antibacterial activity of 3-benzoyl-2-oxo/thioxo-1, 2, 3, 4-tetrahydropyrimidine analogues. 5-Acyl-6-methyl-4-substituted-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidines were synthesized by cyclocondensation reaction between appropriate aldehyde, acetoacetate and urea/thiourea in presence of aluminium chloride and hydrochloric acid which upon treatment with benzoyl chloride in presence of aluminium chloride in presence of pyridine in benzene furnish the title compounds. The compounds have been tested for antibacterial activity against staphylococcus aureus