THROMBOXANE MODULATING AGENTS - 4 - DESIGN AND SYNTHESIS OF HLOROPHENYL)SULFONYL)-AMINO]ETHYL)BENZENEPROPANOIC ACID-DERIVATIVES AS POTENT THROMBOXANE RECEPTOR ANTAGONISTS

Authors
DACK KN DICKINSON RP LONG CJ STEELE J
Citation
Kn. Dack et al., THROMBOXANE MODULATING AGENTS - 4 - DESIGN AND SYNTHESIS OF HLOROPHENYL)SULFONYL)-AMINO]ETHYL)BENZENEPROPANOIC ACID-DERIVATIVES AS POTENT THROMBOXANE RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 8(16), 1998, pp. 2061-2066
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
16
Year of publication
1998
Pages
2061 - 2066
Database
ISI
SICI code
0960-894X(1998)8:16<2061:TMA-4->2.0.ZU;2-V
Abstract
The design of a series of thromboxane receptor antagonists based on ch lorophenyl)sulfonyl}amino]ethyl)benzenepropanoic acid (1) is described . Addition of an arylmethyl group at the 5-position of 1 gave exceptio nally 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 all oral dose of 0.1 mg/kg. (C) 1998 Elsevier Science Ltd. All rights reserved.