Discovery and preliminary SAR of 5-arylidene-2,2-dimethyl-1,3-dioxane- 4,6-diones as platelet aggregation inhibitors

Comb Chem High Throughput Screen. 2012 Aug;15(7):551-4. doi: 10.2174/138620712801619122.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dioxanes / chemical synthesis
  • Dioxanes / chemistry
  • Dioxanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Discovery*
  • High-Throughput Screening Assays
  • Humans
  • Molecular Structure
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemical synthesis
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Dioxanes
  • Platelet Aggregation Inhibitors
  • Meldrum's acid