147332-48-7Relevant articles and documents
Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors: Synthesis and Biological Properties of alkenoic Acids
Faull, Alan W.,Brewster, Andrew G.,Brown, George R.,Smithers, Michael J.,Jackson, Ruth
, p. 686 - 694 (1995)
The design, synthesis, and pharmacology of a new class of compounds possessing bith thromboxane receptor antagonist and thromboxane synthase inhibitory properties are described.Replacement of the phenol group of the known thromboxane antagonist series 4(Z)-6-hex-4-enoic acid by a 3-pyridyl group led to a series of compounds, 5, which were potent thromboxane synthase inhibitors and weak thromboxane antagonists.Further modifications at the dioxane C2 position led to compounds, 7, which were potent dual-acting agents.In the case of compound 7w, the dual activity was shown to reside almost exclusively in the (-)-enantiomer, 7x.Following oral dosing to rats and dogs, 7x (3 mg/kg) displayed significant dual activity over a period of at least 8 h.