Design, Synthesis, and Structure–Activity Relationships of a Novel Series of 5-Alkylidenepyridazin-3 (2 H)-ones with a Non-cAMP-Based Antiplatelet Activity

…, M Yáñez, R Laguna, E Cano, E Sotelo

Index: Coelho, Alberto; Ravina, Enrique; Fraiz, Nuria; Yanez, Matilde; Laguna, Reyes; Cano, Ernesto; Sotelo, Eddy Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6476 - 6484

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Citation Number: 16

Abstract

5-Alkylidenepyridazin-3-ones with four points of diversity (R2, R6, X, Y) have been synthesized and evaluated as platelet aggregation inhibitors. Several derivatives eliciting antiplatelet activity in the low micromolar range (eg, 14e, 14k, 14p, 14v, IC50≅ 1 µ M) were identified. Structure–activity relationships studies on these compounds revealed the key molecular determinants of this new family of antiplatelet agents:(a) two ester groups in the ...