Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles

被引：32

作者：

Shu, Hong ^{[1
]}

Izenwasser, Sari ^{[2
]}

Wade, Dean ^{[2
]}

Stevens, Edwin D. ^{[1
]}

Trudell, Mark L. ^{[1
]}

机构：

[1] Univ New Orleans, Dept Chem, New Orleans, LA 70148 USA

[2] Univ Miami, Sch Med, Dept Psychiat & Behav Sci, Miami, FL USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期

关键词：

Cannabinoid receptors; Triazoles; Click chemistry; FUNCTIONAL EXPRESSION; INVERSE AGONISM; DRUG-ABUSE; RAT-BRAIN; ANTAGONIST; LOCALIZATION; SR141716A;

D O I：

10.1016/j.bmcl.2008.11.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles were synthesized regioselectively using click chemistry and evaluated at CB1 cannabinoid receptors. The n-propyl ester 11 (K-i = 4.6 nM) and phenyl ester 14 ( Ki = 11 nM) exhibited the most potent affinity of the series. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：891 / 893

页数：3

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