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

被引：22

作者：

Cimetière, B ^{[1
]}

Dubuffet, T ^{[1
]}

Landras, C ^{[1
]}

Descombes, JJ ^{[1
]}

Simonet, S ^{[1
]}

Verbeuren, TJ ^{[1
]}

Lavielle, G ^{[1
]}

机构：

[1] Inst Rech Servier, Ctr Rech, F-78290 Croissy Sur Seine, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(98)00221-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 Lf inhibits TXA2 synthase with an IC50 value of 0.64 mu M and the aggregation of human platelets with an IC50 value of 0.063 mu M and shows a long duration of action in different species after oral administration. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1381 / 1386

页数：6

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