THROMBOXANE MODULATING AGENTS .2. THROMBOXANE RECEPTOR ANTAGONISTS DERIVED FROM THE THROMBOXANE SYNTHASE INHIBITOR DAZMEGREL

Authors
DICKINSON RP DACK KN STEELE J TUTE MS
Citation
Rp. Dickinson et al., THROMBOXANE MODULATING AGENTS .2. THROMBOXANE RECEPTOR ANTAGONISTS DERIVED FROM THE THROMBOXANE SYNTHASE INHIBITOR DAZMEGREL, Bioorganic & medicinal chemistry letters, 6(14), 1996, pp. 1691-1696
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
14
Year of publication
1996
Pages
1691 - 1696
Database
ISI
SICI code
0960-894X(1996)6:14<1691:TMA.TR>2.0.ZU;2-V
Abstract
The design of dual thromboxane synthase inhibitor/thromboxane receptor antagonists (e.g, 15) based on the structure of the thromboxane synth ase inhibitor dazmegrel is described. More potent receptor antagonists (e.g, 16c) result from replacement of the pyridinyl subsituent with 4 -fluorophenyl. Modelling suggests the existence of more than one site capable of interacting with the aryl sulfonamide of TxA(2) receptor an tagonists. Copyright (C) 1996 Elsevier Science Ltd