3-Oxo-2-aryl-4-m-chloropheny1-5-tetra-O-acetyl-beta-D-glucopyranosylimino-1,2,4-thiadiazolidines have been prepared by the interaction of 1-aryl-3-m-chloro carbamide and tetra-O-acetyl-beta-D-glucopyranosyl-S-chloro-isothiocarbamoyl chloride. The identities of these newly synthesized compounds are established on the basis of elemental analysis IR, H-1 NMR, C-13 NMR, and mass spectral analysis. These compounds were assayed for their antibacterial and antifungal activity against E. coli, S. aureus, B. cereus, P. aeruginosa, P. vulgaris, A. niger and C. albicans to get potent bioactive molecule.