Synthesis and Pharmacological Activity of C(2)-Substituted Benzimidazoles

Series of new compounds containing 2-pyrrolidinomethyl and 2-piperazinomethyl groups and 2-morpholino and 2-morpholinoethylamine substituents were synthesized. The antiglycation activities of 2-(morpholin-4-yl)-1-(propen-2-en-1-yl)-1H-benzimidazole and 2-(morpholin-4-yl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole were comparable to that of aminoguanidine. Some compounds exhibited moderate antiserotonin, anti-angiotensin, antioxidant, and dipeptidyl peptidase-4 (DPP-4) inhibitory effects.