Significant Discovery of Tetrahydrothieno[3,2‐c]pyridine‐2‐carboxamide Analogs as Potent P2Y12 Receptor Antagonists

A series of analogs containing tetrahydrothieno[3,2‐c]pyridine‐2‐carboxamide as a building block with numerous alicyclic and aromatic amines were synthesized. All analogs were characterized by spectral analysis and evaluated for their in vitro antiplatelet activity. 4‐Fluorophenyl amide derivatives (compounds 8 – 11 ) have been found to be most active in the series with respect to prasugrel and aspirin, a third generation antiplatelet agents (P2Y12 receptor antagonists). Docking study also manifested the admirable binding mode of in vitro active compounds 10 and 11 with the target protein. The results may provide a new perception for future pharmacophore with simple design strategy and avoid tedious synthesis of clopidogrel and prasugrel.