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Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation

หน่วยงาน Central Drug Research Institute (CDRI), India

รายละเอียด

ชื่อเรื่อง : Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation
นักวิจัย : Kumar K S, Anil , Misra, Ankita , Siddiqi, T I , Srivastava, Stuti , Jain, Manish , Bhatta, R S , Barthwal, M K , Dikshit, Madhu , Dikshit, D K
คำค้น : Thrombosis , Antiplatelet , Pyroglutamic Acid , Aminomethylpiperidine , Collagen , Epinephrine
หน่วยงาน : Central Drug Research Institute (CDRI), India
ผู้ร่วมงาน : -
ปีพิมพ์ : 2557
อ้างอิง : European Journal of Medicinal Chemistry. 2014, 81, 456-72 , http://hdl.handle.net/123456789/1387
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : CSIR-CDRI Communication No. 8694
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

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.

บรรณานุกรม :
Kumar K S, Anil , Misra, Ankita , Siddiqi, T I , Srivastava, Stuti , Jain, Manish , Bhatta, R S , Barthwal, M K , Dikshit, Madhu , Dikshit, D K . (2557). Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation.
    : Central Drug Research Institute (CDRI), India.
Kumar K S, Anil , Misra, Ankita , Siddiqi, T I , Srivastava, Stuti , Jain, Manish , Bhatta, R S , Barthwal, M K , Dikshit, Madhu , Dikshit, D K . 2557. "Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation".
    : Central Drug Research Institute (CDRI), India.
Kumar K S, Anil , Misra, Ankita , Siddiqi, T I , Srivastava, Stuti , Jain, Manish , Bhatta, R S , Barthwal, M K , Dikshit, Madhu , Dikshit, D K . "Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation."
    : Central Drug Research Institute (CDRI), India, 2557. Print.
Kumar K S, Anil , Misra, Ankita , Siddiqi, T I , Srivastava, Stuti , Jain, Manish , Bhatta, R S , Barthwal, M K , Dikshit, Madhu , Dikshit, D K . Synthesis and Identification of Chiral Aminomethylpiperidine Carboxamides as Inhibitor of Collagen Induced Platelet Activation. : Central Drug Research Institute (CDRI), India; 2557.