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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Evaluation of Bridged Analogues of the Platelet Aggregation Inhibitor Trifenagrel

Author(s): Magdalena Slusarczyk, Wim M. De Borggraeve, Georges Hoornaert, Koen Robeyns, Luc Van Meervelt, Tongfei Wu, Frederik Deroose and Joannes T.M. Linders

Volume 6, Issue 7, 2009

Page: [478 - 486] Pages: 9

DOI: 10.2174/157018009789108213

Price: $65

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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