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New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors

Authors :
Cimetière, Bernard
Dubuffet, Thierry
Landras, Caroline
Descombes, Jean-Jacques
Simonet, Serge
Verbeuren, Tony J.
Lavielle, Gilbert
Source :
Bioorganic & Medicinal Chemistry Letters; June 1998, Vol. 8 Issue: 11 p1381-1386, 6p
Publication Year :
1998

Abstract

A pyridine group was linked to the tetrahydronaphthalene moiety of the derivatives described in the preceding paper, to afford new combined thromboxane receptor (TP-receptor) antagonists and synthase inhibitors. The most interesting compound 2finhibits TXA2 synthase with an IC50 value of 0.64 μM and the aggregation of human platelets with an IC50 value of 0.063 μM and shows a long duration of action in different species after oral administration.

Details

Language :
English
ISSN :
0960894X and 14643405
Volume :
8
Issue :
11
Database :
Supplemental Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Periodical
Accession number :
ejs3513064
Full Text :
https://doi.org/10.1016/S0960-894X(98)00221-2