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Discovery and Preliminary SAR of 5-Arylidene-2,2-Dimethyl-1,3-Dioxane- 4,6-Diones as Platelet Aggregation Inhibitors

Abstract:

We herein document the discovery of 5-arylidene-2,2-dimethyl-1,3-dioxane-4,6-diones as a novel family of platelet aggregation inhibitors. The preliminary optimization study enabled us to establish the most salient features of the structure-activity relationships in this series as well as to identify novel derivatives that are upto 60 times more potent than the hit structure 1 and slightly superior to the reference drug Milrinone.

Authors:   El Maatougui, Abdelaziz; JhonnyAzuaje,; Coelho, Alberto; Cano, Ernesto; Yanez, Matilde; Lopez, Carmen; Yaziji, Vicente; Carbajales, Carlos; Sotelo, Eddy
Journal:   Combinatorial Chemistry
DOI:   10.2174/138620712801619122

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