A class of novel N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-substituted sulfonamide 3(a-f) and methyl (2'-(1Htetrazol- 5-yl)biphenyl-4-yl)-substituted carbamate 5(a-d) derivatives were synthesized from (2'-(1H-tetrazol-5-yl)- biphenyl-4-yl)methanamine, an important drug intermediate and using pharmacologically active functionalized sulfonyl chlorides and carbonochloridates in presence of mild basic conditions respectively. The structures of all the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analysis. The title compounds were screened for antibacterial activity against two gram positive bacterial strains such as Staphylococcus aureus (ATCC-29737) and Bacillus subtilis (ATCC-6633) and two gram negative bacterial strains such as Escherichia coli (ATCC-2343) and Pseudomonas aeruginosa (MTCC-1034) and also screened for antifungal activity against Fusarium oxysporum, Candida albicans and Aspergillus niger pathogens. Compounds 3a and 5a exhibited potent activity and remaining derivatives showed moderate activity against bacteria and fungi.