Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[{(4- chlorophenyl)sulfonyl}-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(98)00242-X

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.