Title: Synthesis and Biological Evaluation of Bridged Analogues of the Platelet Aggregation Inhibitor Trifenagrel
Authors: Slusarczyk, Magdalena
De Borggraeve, Wim ×
Hoornaert, Georges
Robeyns, Koen
Van Meervelt, Luc
Wu, Tongfei
Deroose, Frederik
Linders, Joannes T. M #
Issue Date: Oct-2009
Publisher: Bentham science publ ltd
Series Title: Letters in drug design & discovery vol:6 issue:7 pages:478-486
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.
ISSN: 1570-1808
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Design and Synthesis
Chemistry - miscellaneous
Biochemistry, Molecular and Structural Biology Section
× corresponding author
# (joint) last author

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