Present study describes the synthesis of a novel series of 3,5-diiodo-4-(5-nitro-1H-2-imidazolyl)benzoyl amino acids and di/tri/tetrapeptides using diisopropylcarbodiimide/dicyclohexylcarbodiimide (DIPC/DCC) as coupling agents and N-methylmorpholine/triethylamine (NMM/TEA) as bases. Structure elucidation of all the newly synthesized compounds was done by elemental analysis and IR, 1H NMR, 13C NMR and mass spectral data. Synthesized imidazolopeptides were screened for their anthelmintic activity and found to possess moderate to good bioactivity against earthworms Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugeniea when compared to reference drugs - albendazole and mebendazole at dose level of 2 mg mL−1.