A new series of novel 2-oxo-6-(5-methyl-[1,3,4]-thiadiazol-2-yl sulfanylmethyl)-1, 2, 3, 4-tetrahydropyrimidine derivatives (3a-h) were synthesized by Biginelli reaction and characterized by elemental, IR, 1H NMR, 13C NMR and Mass spectral analysis . All the compounds were screened for their in vitro antibacterial activity (B.Subtilis, Staphylococcus aereus, E.coli, K.pneumonia) and antifungal activity (C.albicans, A.niger) by disc diffussion method. Among the tested compounds showed the significant antimicrobial activity. The newly synthesized compounds were docked with glucosamine-6-phosphate synthase enzyme in order to study the accepted binding mode of the active compounds.