Combinatorial synthesis of SSAO inhibitors using Sonogashira coupling: SAR of aryl propargylic amines

被引：9

作者：

Conn, C ^{[1
]}

Shimmon, R ^{[1
]}

Cordaro, F ^{[1
]}

Hargraves, TL ^{[1
]}

Ibrahim, P ^{[1
]}

机构：

[1] Univ Technol Sydney, Dept Chem Mat & Forens Sci, Sydney, NSW 2007X, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(01)00506-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationships for semicarbazide-sensitive amine oxidase (SSAO) inhibitors based on arylpropynylamines was investigated using solution-phase combinatorial Sonogashira coupling. The results suggest that binding to the active site occurs by coordination of the amine to the proximal copper(II) and formation of a pi -complex between topaquinone and the electron-rich aryl group of the inhibitor. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2565 / 2568

页数：4

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