Abstract
The synthesis and preliminary biological investigation of three methylene bridged heterocyclic analogues of trifenagrel, a potent inhibitor of arachidonate-induced aggregation of platelets, is reported. The synthesis of the compounds is based on the cyclocondensation reaction of a tricyclic 1,2-diketone with an appropriate aldehyde, hydrazide or a diamine to form an imidazole, a 1,2,4-triazine or a pyrazine moiety respectively. In comparison to trifenagrel, its methylene- bridged analogue had much reduced activity, while its pyrazine analogue was devoid of activity.
Letters in Drug Design & Discovery
Title: Synthesis and Biological Evaluation of Bridged Analogues of the Platelet Aggregation Inhibitor Trifenagrel
Volume: 6 Issue: 7
Author(s): Magdalena Slusarczyk, Wim M. De Borggraeve, Georges Hoornaert, Koen Robeyns, Luc Van Meervelt, Tongfei Wu, Frederik Deroose and Joannes T.M. Linders
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Abstract: The synthesis and preliminary biological investigation of three methylene bridged heterocyclic analogues of trifenagrel, a potent inhibitor of arachidonate-induced aggregation of platelets, is reported. The synthesis of the compounds is based on the cyclocondensation reaction of a tricyclic 1,2-diketone with an appropriate aldehyde, hydrazide or a diamine to form an imidazole, a 1,2,4-triazine or a pyrazine moiety respectively. In comparison to trifenagrel, its methylene- bridged analogue had much reduced activity, while its pyrazine analogue was devoid of activity.
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Slusarczyk Magdalena, De Borggraeve M. Wim, Hoornaert Georges, Robeyns Koen, Meervelt Van Luc, Wu Tongfei, Deroose Frederik and Linders T.M. Joannes, Synthesis and Biological Evaluation of Bridged Analogues of the Platelet Aggregation Inhibitor Trifenagrel, Letters in Drug Design & Discovery 2009; 6 (7) . https://dx.doi.org/10.2174/157018009789108213
DOI https://dx.doi.org/10.2174/157018009789108213 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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