DESIGN OF DUAL-ACTING THROMBOXANE ANTAGONIST-SYNTHASE INHIBITORS BY AMUTUAL PRODRUG APPROACH

Authors
BROWN GR CLARKE DS FAULL AW FOUBISTER AJ SMITHERS MJ
Citation
Gr. Brown et al., DESIGN OF DUAL-ACTING THROMBOXANE ANTAGONIST-SYNTHASE INHIBITORS BY AMUTUAL PRODRUG APPROACH, Bioorganic & medicinal chemistry letters, 6(3), 1996, pp. 273-278
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
3
Year of publication
1996
Pages
273 - 278
Database
ISI
SICI code
0960-894X(1996)6:3<273:DODTAI>2.0.ZU;2-H
Abstract
A mutual prodrug approach to dual acting thromboxane receptor antagoni st - thromboxane synthase inhibitor compounds is reported in which TXA (2) antagonist and inhibitory 19-dioxanes with hexenoic acid side chai ns, were linked by diester and diamide groups. When linking of the com ponents was achieved via di O-alkyl carboxylic esters of catechol, bot h TXA(2) receptor antagonist activity and TXA(2) synthase inhibition w ere observed for a single enantiomer (16) in ex vivo tests following o ral dosing to dogs at 5 mg/kg.