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Synthesis and evaluation of anti-thrombotic activity of benzocoumarin amide derivatives

  作者 Sashidhara, KV; Palnati, GR; Avula, SR; Singh, S; Jain, M; Dikshit, M  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-9;  页码  3115-3121  
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[摘要]A series of novel benzocoumarin amide derivatives have been synthesized and evaluated for their antithrombotic activity. Amongst these, compounds 5, 7 and 8 exhibited promising anti-thrombotic profile in an established model of mouse thrombosis. Hence, comprehensive profiling on platelet aggregation and coagulation parameters was carried out to assess its potential as a lead candidate. In vitro treatment of these compounds in mice plasma resulted into significant reduction in ADP (p < 0.01) and collagen (p < 0.001) induced platelet aggregation. Moreover, Compounds 5, 7 and 8 also significantly increased thrombin time (p < 0.05). Thus, in the present study, these benzocoumarin amide derivatives exhibited anti-thrombotic profile via both anti-platelet as well as anti-coagulant action. (C) 2012 Elsevier Ltd. All rights reserved.

 
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