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.
Keywords: Antiplatelet agents, Meldrum´s acid, platelet aggregation inhibitors, SAR, 5-Arylidene-2, 2-Dimethyl-1, 3-Dioxane-4, 6-Diones, Milrinone, antithrombotic agents, novel chemotypes, chemical genomics, signal transduction
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Published on: 01 July, 2012
Page: [551 - 554]