As a result of our continuing study aimed at the discovery and development of novel antiplatelet agents, 1-benzyl-2-(5-methyl-2-furyl) benzimidazole (A) was synthesized and evaluated for its antiplatelet activity. The preliminary results of compound A showed good inbibitory effect on collagen, arachidonic acid, U46619-induced platelet aggregation, it can be developed as a new category of drug to treat thrombosis. Encourage by this results, compound A was selected as a lead compound in this article. Two target analogs of benzimidazole were designed, they are 5-substituted-1-substisutedbenzyl-2-(5-methyl-2-furyl) benzimidazole (1-17) and 3-substituted-2-(5-methyl-2-furyl)imidazo [4,5-b]pyridine (19-71).
In this article, we aim at synthesizing and evaluating their antiplatelet activities. Some of the target compounds showed the same pattern as compound A and exhibit highly inhibitory activity against platelet aggregation induced by collagen. The finding will add to our understanding of SAR of benzimidazoles. The goal of our continuing studies is to identify novel compounds for antiplatelet study.