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Title: Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation
Authors: Kumar K S, Anil
Misra, Ankita
Siddiqi, T I
Srivastava, Stuti
Jain, Manish
Bhatta, R S
Barthwal, M K
Dikshit, Madhu
Dikshit, D K
Keywords: Thrombosis;Antiplatelet;Pyroglutamic Acid;Aminomethylpiperidine;Collagen;Epinephrine
Issue Date: 2014
Description: A series of chiral lactamcarboxamides 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 hours and points to its excellent bioavailability. The compounds 31a (IC50= 6.6µM) and 32a (IC50=37µM), as well as their racemic mixture 28i (IC50=16µM) significantly inhibited collagen-induced human platelet aggregation in vitro. Compound 34c displayed dual mechanism of action against both collagen (IC50=3.3µM) and U46619 (IC50=2.7M) induced platelet aggregation. The pharmacokinetic study of 31a indicated very faster absorption, prolonged and constant systemic exposure and thereby exhibiting better therapeutic response.
Other Identifiers: European Journal of Medicinal Chemistry. 2014, 81, 456-72
Appears in Collections:Medicinal and Process Chemistry

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