The present work describe a safe, mild, eco-friendly and versatile method for the synthesis of N1,N1,N4,N4-tetramethylpiperazine-1,4-dicarboxamide. The prepared compound was screened against Aedes caspius (Pallas) and Culex pipiens (Linnaeus) larvae and compared to its parent piperazine moiety. Likewise, histological structure of gut of treated third instar larva was considerably disturbed. The results demonstrated that substituted urea (1,4-dicarboxamide) meddled with the development of the mosquitoes, and had its strongest poisonous impact at 200 ppm for 48 h.