Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Joannes T.M. Linders.

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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Article Details

VOLUME: 6
ISSUE: 7
Year: 2009
Page: [478 - 486]
Pages: 9
DOI: 10.2174/157018009789108213
Price: $58