Synthesis, Biological and Molecular Docking Study of Benzimidazole‐Clubbed Tetrahydrothieno [3, 2‐c] Pyridine as Platelet Inhibitors

Abstract

AbstractTwo novel series of tetrahydrothienopyridine clubbed benzimidazole hybrids were synthesized, characterized by spectral studies 1H NMR, IR and mass analysis. Synthesized analogs were screened for in vitro antiplatelet activity. In addition, active analogs were further subjected in presence of proton pump inhibitors against standard prasugrel and aspirin to check minimization in antiplatelet activity. Active analogs 1‐(2‐(1‐methyl‐1H‐benzo[d]imidazol‐2‐yl)‐6,7‐dihydrothieno[3,2‐c]pyridin‐5(4H)‐yl)ethan‐1‐one (11) and (2‐(1‐(2‐fluorobenzyl)‐1H‐benzo[d]imidazol‐2‐yl)‐6,7‐dihydrothieno[3,2‐c]pyridin‐5(4H)‐yl)(3,4,5‐trichlorophenyl)methanone (25) were significantly found more active than the standards in the presence of proton pump inhibitors. The structure and antiplatelet activity relationship was supported by molecular docking studies of active analogs to know how effectively, activity influenced by the merger of proton pump inhibitor precursor benzimidazole. The above studies successfully revealed that the synthesized analogs may found more active with further amendments via pharmacological point of view.