Bioorganic and Medicinal Chemistry Letters p. 2061 - 2066 (1998)
Update date:2022-08-05
Topics:
Dack, Kevin N.
Dickinson, Roger P.
Long, Clive J.
Steele, John
The design of a series of thromboxane receptor antagonists based on 3- (2-[{(4-chlorophenyl)sulfonyl}amino]ethyl)benzenepropanoic acid (1) is described. Addition of an arylmethyl group at the 5-position of 1 gave exceptionally potent agents in vitro and in vivo, with 13a (UK-147,535) giving complete blockade of the TxA2 receptor for greater than 12 hours in dogs, following an oral dose of 0.1 mg/kg.
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