Journal of Medicinal Chemistry p. 686 - 694 (1995)
Update date:2022-08-04
Topics:
Faull, Alan W.
Brewster, Andrew G.
Brown, George R.
Smithers, Michael J.
Jackson, Ruth
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-<(4RS,5SR)-4-(2-hydroxyphenyl)-1,3-dioxan-5-yl>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.
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