Abstract: Based on the recently reported structure of highly active mesoionic nAChR modulators, 30 novel benzopyrazole compounds were designed and synthesized through scaffold hopping. Their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. Insecticidal activity assays revealed compounds A1 , A7 , A16 and A22 showed about 40% mortality against Aphis craccivora at the concentration of 500 mg/L, however still less active than lead compound 1 . Preliminary analysis suggests similar binding modes for mesoionic and non-mesoionic structures, and the differences in their physicochemical properties and electrostatic potential surface between A1 and compound 1 may be the main reason for the lower activities of the target compounds than that of compound 1 .