title: Synthesis and evaluation of anti-thrombotic activity of benzocoumarin amide derivatives.
abstract: A series of novel benzocoumarin amide derivatives have been synthesized and evaluated for their anti-thrombotic 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.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR-CDRI, Lucknow 226 001, India. sashidhar123@gmail.com
authors.forename: Koneni V
authors.initials: KV
authors.lastname: Sashidhara
authors.forename: Gopala Reddy
authors.initials: GR
authors.lastname: Palnati
authors.forename: Srinivasa Rao
authors.initials: SR
authors.lastname: Avula
authors.forename: Surendra
authors.initials: S
authors.lastname: Singh
authors.forename: Manish
authors.initials: M
authors.lastname: Jain
authors.forename: Madhu
authors.initials: M
authors.lastname: Dikshit
mesh_terms: D000244:Adenosine Diphosphate / Q000494:pharmacology; D000818:Animals; D003094:Collagen / Q000494:pharmacology; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013918:Thrombin Time
chemical_list: D003374:Coumarins; D005343:Fibrinolytic Agents; D010975:Platelet Aggregation Inhibitors; D000244:Adenosine Diphosphate; D003094:Collagen