Design,green synthesis and pharmacological evaluation of novel 5,6-diaryl-1,2,4-triazines bearing 3-morpholinoethylamine moiety as potential antithrombotic agents* |
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| Authors: | Riyaj S Tamboli Rajani Giridhar Hardik P Gandhi Ashish M Kanhed Hemant M Mande |
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| Institution: | 1. Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, India and;2. Department of Chemistry, Faculty of Science, Sayajiganj, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, India |
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| 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. |
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| Keywords: | 1 2 4-Triazines antithrombotic agents antiplatelet agents aspirin green synthesis molecular docking |
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