Combined tachykinin receptor antagonist: Synthesis and stereochemical structure-activity relationships of novel morpholine analogues

被引：24

作者：

Nishi, T

Ishibashi, K

Takemoto, T

Nakajima, K

Fukazawa, T

Iio, Y

Itoh, K

Mukaiyama, O

Yamaguchi, T

机构：

[1] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan

[2] Sankyo Co Ltd, Neurosci & Immunol Res Labs, Shinagawa Ku, Tokyo 1408710, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(00)00324-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 exhibited high binding affinities for NK1, NK2 and NK3 receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1665 / 1668

页数：4

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