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
收藏
页码：1381 / 1386
页数：6
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