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

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.

Cite this article as:

El Maatougui Abdelaziz, JhonnyAzuaje , Coelho Alberto, Cano Ernesto, Yanez Matilde, Lopez Carmen, Yaziji Vicente, Carbajales Carlos and Sotelo Eddy, Discovery and Preliminary SAR of 5-Arylidene-2,2-Dimethyl-1,3-Dioxane- 4,6-Diones as Platelet Aggregation Inhibitors, Combinatorial Chemistry & High Throughput Screening 2012; 15(7) . https://dx.doi.org/10.2174/138620712801619122