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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dioxanes / chemical synthesis
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Dioxanes / chemistry
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Dioxanes / pharmacology*
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Dose-Response Relationship, Drug
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Drug Discovery*
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High-Throughput Screening Assays
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Humans
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Molecular Structure
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Platelet Aggregation / drug effects*
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Platelet Aggregation Inhibitors / chemical synthesis
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Dioxanes
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Platelet Aggregation Inhibitors
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Meldrum's acid