title: 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.affiliation: Center for Research in Chemical Biology and Molecular Materials, University of Santiago de Compostela, Santiago de Compostela, 15782, Spain.
authors.forename: Abdelaziz
authors.initials: A
authors.lastname: El Maatougui
authors.forename: Jhonny
authors.initials: J
authors.lastname: Azuaje
authors.forename: Alberto
authors.initials: A
authors.lastname: Coelho
authors.forename: Ernesto
authors.initials: E
authors.lastname: Cano
authors.forename: Matilde
authors.initials: M
authors.lastname: Yañez
authors.forename: Carmen
authors.initials: C
authors.lastname: López
authors.forename: Vicente
authors.initials: V
authors.lastname: Yaziji
authors.forename: Carlos
authors.initials: C
authors.lastname: Carbajales
authors.forename: Eddy
authors.initials: E
authors.lastname: Sotelo
mesh_terms: D004146:Dioxanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D057166:High-Throughput Screening Assays; D006801:Humans; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004146:Dioxanes; D010975:Platelet Aggregation Inhibitors; C076489:Meldrum's acid