Details

Autor(en) / Beteiligte

• Dack, Kevin N.
• Dickinson, Roger P.
• Long, Clive J.
• Steele, John

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (16), p.2061-2066

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

1998

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• 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 TxA 2 receptor for greater than 12 hours in dogs, following an oral dose of 0.1 mg/kg. 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 13â (UK-147,535) giving complete blockade of the TxA 2 receptor for greater than 12 hours in dogs, following an oral dose of 0.1 mg/kg.