Synthesis and biological evaluation of bridged analogues of the platelet aggregation inhibitor trifenagrel
(2009) Letters in Drug Design & Discovery — Vol. 6, n° 7, p. 478-486 (2009)
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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. © 2009 Bentham Science Publishers Ltd.
- Affiliations
KU LEUVEN Department of Chemistry
Citations
Slusarczyk, M., De Borggraeve, W. M., Hoornaert, G., Robeyns, K., Van Meervelt, L., Wu, T., Deroose, F., & Linders, J. T. M. (2009). Synthesis and biological evaluation of bridged analogues of the platelet aggregation inhibitor trifenagrel. Letters in Drug Design & Discovery, 6(7), 478-486. https://doi.org/10.2174/157018009789108213 (Original work published 2009)