Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists

被引：11

作者：

Mah, R ^{[1
]}

Gerspacher, M

von Sprecher, A

Stutz, S

Tschinke, V

Anderson, GP

Bertrand, C

Subramanian, N

Ball, HA

机构：

[1] Novartis Pharma AG, Pharma Res, CH-4002 Basel, Switzerland

[2] Speedel Expt AG, CH-4123 Allschwil, Switzerland

[3] Univ Melbourne, Dept Pharmacol, Parkville, Vic 3052, Australia

[4] Roche Biosci, Inflammatory Dis Unit, Palo Alto, CA USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(02)00382-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In a continuation of our efforts to simplifly the structure of our neurokinin antagonists, a series of substituted biphenyl derivatives has been prepared. Several compounds exhibit potent affinities for both the NK1 receptor (< 10 nM) and for the NK2 receptor (< 50 nM). Details on the design, synthesis, biological activities, SAR and conformational analysis of this new class of dual NK1/NK2 receptor antagonists are presented. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2065 / 2068

页数：4

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