title: Design, green synthesis and pharmacological evaluation of novel 5,6-diaryl-1,2,4-triazines bearing 3-morpholinoethylamine moiety as potential antithrombotic agents (.).
abstract: The aim of this research work was to investigate a series of novel 5,6-diaryl-1,2,4-triazines (3a-3q) containing 3-morpholinoethylamine side chain, and to address their antiplatelet activity by in vitro, ex vivo and in vivo methods. All compounds were synthesized by environment benign route and their structures were unambiguously confirmed by spectral data. Compounds (3l) and (3m) were confirmed by their single crystal X-ray structures. Out of all the synthesized compounds, 10 were found to be more potent in vitro than aspirin; six of them were found to be prominent in ex vivo assays and one compound (3d) was found to have the most promising antithrombotic profile in vivo. Moreover, compound (3d) demonstrated less ulcerogenicity in rats as compared to aspirin. The selectivity of the most promising compound (3d) for COX-1 and COX-2 enzymes was determined with the help of molecular docking studies and the results were correlated with the biological activity.
authors.affiliation: a Pharmacy Department, Faculty of Technology and Engineering , Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India and.
authors.forename: Riyaj S
authors.initials: RS
authors.lastname: Tamboli
authors.affiliation: a Pharmacy Department, Faculty of Technology and Engineering , Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India and.
authors.forename: Rajani
authors.initials: R
authors.lastname: Giridhar
authors.affiliation: a Pharmacy Department, Faculty of Technology and Engineering , Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India and.
authors.forename: Hardik P
authors.initials: HP
authors.lastname: Gandhi
authors.affiliation: a Pharmacy Department, Faculty of Technology and Engineering , Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India and.
authors.forename: Ashish M
authors.initials: AM
authors.lastname: Kanhed
authors.affiliation: b Department of Chemistry, Faculty of Science , Sayajiganj, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India.
authors.forename: Hemant M
authors.initials: HM
authors.lastname: Mande
authors.affiliation: a Pharmacy Department, Faculty of Technology and Engineering , Kalabhavan, The Maharaja Sayajirao University of Baroda , Vadodara , Gujarat , India and.
authors.forename: Mange Ram
authors.initials: MR
authors.lastname: Yadav
mesh_terms: D000818:Animals; D001792:Blood Platelets / Q000187:drug effects; D015195:Drug Design; D005260:Female; D005343:Fibrinolytic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D062105:Molecular Docking Simulation; D008981:Molsidomine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010973:Platelet Adhesiveness / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D005343:Fibrinolytic Agents; D014227:Triazines; C093444:1,2,4-triazine; C002385:linsidomine; D008981:Molsidomine
keywords: 1,2,4-Triazines; antiplatelet agents; antithrombotic agents; aspirin; green synthesis; molecular docking