Title:Discovery and Preliminary SAR of 5-Arylidene-2,2-Dimethyl-1,3-Dioxane- 4,6-Diones as Platelet Aggregation Inhibitors
Volume: 15
Issue: 7
Author(s): Abdelaziz El Maatougui, JhonnyAzuaje, Alberto Coelho, Ernesto Cano, Matilde Yanez, Carmen Lopez, Vicente Yaziji, Carlos Carbajales and Eddy Sotelo
Affiliation:
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
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.