A series of acetamides have been synthesized and evaluated as potential antipsychotic agents. The target compounds (3a-e) were prepared by reaction of substituted anilines with chloroacetylchloride which further treated with benzyl or benzoyl piperazine in presence of potassium carbonate and potassium iodide as catalyst in acetonitrile. The structures of the target compounds (3a-e) were characterized on the basis of their M.P., TLC, IR and 1H-NMR data. Computational studies of target compounds (3a-e) were carried out by using software programs. The target compounds showed good similarity with respect to standard drugs. The target compounds (3a-e) showed inhibition of 5-HTP induced head twitches behavior and low induction of catalepsy in mice.