In the present work, we have discussed the synthesis of a series of 1-((2'-(2-(2-(substitutedphenyl))-2-oxoethyl)-2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)piperidine-4-carboxylic acid derivatives by the reaction of 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)piperidine-4-carboxylic acid with phenacyl bromides using potassium carbonate. The structures of synthesized derivatives have been characterized using different spectroscopic techniques like FT-IR, ¹H-NMR, ¹³C-NMR, and Mass. Synthesized compounds were screened for their antibacterial and anti-TB activities all the compounds have found better activity against selected pathogenic strains. In addition, in silco molecular docking studies were carried out on targeted enzymes DNA gyrase and 3-oxoacyl-ACP reductase with ADME-toxicology studies.