Synthesis and identification of chiral aminomethylpiperidine carboxamides as inhibitor of collagen induced platelet activation

KSA Kumar, A Misra, TI Siddiqi, S Srivastava…

Index: Anil Kumar; Misra, Ankita; Siddiqi, Tanveer Irshad; Srivastava, Stuti; Jain, Manish; Bhatta, Rabi Sankar; Barthwal, Manoj; Dikshit, Madhu; Dikshit, Dinesh K. European Journal of Medicinal Chemistry, 2014 , vol. 81, p. 456 - 472

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Citation Number: 5

Abstract

Abstract 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 (IC 50= 6.6 ...