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.
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
Combinatorial Chemistry & High Throughput Screening
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.
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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
DOI https://dx.doi.org/10.2174/138620712801619122 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |

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