87341-37-5Relevant academic research and scientific papers
Synthesis and evaluation of dual antiplatelet activity of bispidine derivatives of N-substituted pyroglutamic acids
Misra, Ankita,Anil Kumar,Jain, Manish,Bajaj, Kirti,Shandilya, Shyamali,Srivastava, Smriti,Shukla, Pankaj,Barthwal, Manoj K.,Dikshit, Madhu,Dikshit, Dinesh K.
, p. 1 - 12 (2016)
N-aralkylpyroglutamides of substituted bispidine were prepared and evaluated for their ability to inhibit collagen induced platelet aggregation, both in vivo and in vitro. Some compounds showed high anti-platelet efficacy (in vitro) of which six inhibited
Synthesis and identification of chiral aminomethylpiperidine carboxamides as inhibitor of collagen induced platelet activation
Anil Kumar,Misra, Ankita,Siddiqi, Tanveer Irshad,Srivastava, Stuti,Jain, Manish,Bhatta, Rabi Sankar,Barthwal, Manoj,Dikshit, Madhu,Dikshit, Dinesh K.
, p. 456 - 472 (2014/06/09)
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.
