European Journal of Medicinal Chemistry p. 456 - 472 (2014)
Update date:2022-08-15
Topics: Synthesis NMR spectroscopy Chiral Mass spectrometry carboxamides High-performance liquid chromatography (HPLC) Inhibitor Chemical Synthesis Identification Aminomethylpiperidine Collagen Platelet activation
Anil Kumar
Misra, Ankita
Siddiqi, Tanveer Irshad
Srivastava, Stuti
Jain, Manish
Bhatta, Rabi Sankar
Barthwal, Manoj
Dikshit, Madhu
Dikshit, Dinesh K.
A series of chiral lactam carboxamides of aminomethylpiperidine were synthesized and investigated for the collagen induced in vitro anti-platelet efficacy and collagen plus epinephrine induced in vivo pulmonary thromboembolism. The compound 31a (30 μM/kg) displayed a remarkable antithrombotic efficacy (60% protection) which was sustained for more than 24 h and points to its excellent bioavailability. The compounds 31a (IC50 = 6.6 μM) and 32a (IC50 = 37 μM), as well as their racemic mixture 28i (IC50 = 16 μM) significantly inhibited collagen-induced human platelet aggregation in vitro. Compound 34c displayed dual mechanism of action against both collagen (IC50 = 3.3 μM) and U46619 (IC50 = 2.7 μM) induced platelet aggregation. The pharmacokinetic study of 31a indicated very faster absorption, prolonged and constant systemic exposure and thereby exhibiting better therapeutic response.
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