A series of new [1,2,4]triazolo[4,3-c]quinazoline linked with piperazine scaffolds 8(a-j) were synthesized and evaluated for their antibacterial activity against Gram-positive bacteria (B. subtilis, S. aureus, M. luteus), Gram-negative bacteria (P. vulgaris, S. typhimurium, E. coli). Antibacterial evaluation indicates, the compounds containing 2-chlorophenyl (8d) showed better activity against S. aureus and M. Luteus, 4-chlorophenyl (8e) showed better activity against Gram-positive and Gram-negative bacteria (except E. coli). Similarly, compounds containing 4-nitrophenyl (8h) was active against all the tested strains except S. Aureus. The other compounds also exhibited considerable antibacterial activities.