Synthesis and evaluation of anti-thrombotic activity of benzocoumarin amide derivatives
作者:Koneni V. Sashidhara、Gopala Reddy Palnati、Srinivasa Rao Avula、Surendra Singh、Manish Jain、Madhu Dikshit
DOI:10.1016/j.bmcl.2012.03.059
日期:2012.5
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.