A series of novel non-peptide diamide compounds was synthesized and evaluated as antibradykinin agents by utilizing guinea-pig ileum smooth muscle. Among the final compounds,(Z)-4-(4-(bis (4-fluorophenyl) methyl) piperazin-1-yl)-4-oxo-N-(4-phenylbutan-2- yl) but-2-enamide showed most favorable bradykinin inhibitory activity and demonstrated analgesic efficacies in the rat models of inflammatory and neuropathic pain.
