Sugar isocyanates are important reagents in medicinal/pharmaceutical chemistry. Some sugar isothiobiurets and isodithiobiurets show potential antimicrobial activities. Looking at the importance of these compounds we plan the synthesis of 1-aryl-5-tetra-O-benzoyl-b-D-glucosyl-2-S-benzyl-2-isothiobiurets. Several 1-aryl-5-tetra-O-benzoyl-b- D-glucosyl-2-S-benzyl-2-isothiobiurets have been synthesized by the interaction of tetra-O-benzoyl-b-D-glucosyl isocyanate with 1-aryl-S-benzyl isothiocarbamides. These compounds were screened for their in vitro antibacterial and antifungal activity against E. coli, S. aureus, P.vulgaris, B. cereus, P. aeruginosa, A. niger and C. albicans respectively. The identities of these newly synthesized compounds are established on the basis of usual chemical transformations and IR, 1H NMR, and Mass spectral studies.