The synthesis of a novel thromboxane receptor antagonist 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1,3-dioxan-cis-5-yl) hexenoic acid ICI 192605

  • Prostaglandins. 1988 Aug;36(2):173-8. doi: 10.1016/0090-6980(88)90304-8.
A G Brewster  1 ,  G R Brown ,  A J Foubister ,  R Jessup ,  M J Smithers
Affiliations
  • 1. Research Department 2, ICI Pharmaceuticals, Macclesfield, Cheshire, England.
PMID: 2973084 DOI: 10.1016/0090-6980(88)90304-8
Abstract

The synthesis and summary pharmacology of a novel thromboxane receptor antagonist 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1, 3-dioxan-cis-5-yl) hexenoic acid (3) is reported. Compound 3 was competitive and selective with pA2 values of 8.0 +/- 0.1 (rabbit) and 8.4 +/- 0.05 (rat) on smooth muscle preparations and 8.16 +/- 0.01 on human platelets. In vivo activity of 3 was demonstrated in a Konzett Rossler guinea pig model at 0.01 mg/kg p.o.

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