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Significant Discovery of Tetrahydrothieno[3,2‐ c ]pyridine‐2‐carboxamide Analogs as Potent P2Y12 Receptor Antagonists
Author(s) -
Bhalekar Sujit B.,
Shelke Sharad N.
Publication year - 2019
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201800550
Subject(s) - pharmacophore , chemistry , carboxamide , prasugrel , amide , stereochemistry , pyridine , alicyclic compound , combinatorial chemistry , clopidogrel , medicinal chemistry , aspirin , biochemistry , organic chemistry
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.