4-烷氧羰基-1,5-二芳基-1,2,3-三唑的合成及 CB1 cannabinoid 受体亲和力。
Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles.
机构信息
Department of Chemistry, University of New Orleans, 2000 Lakeshore Drive, New Orleans, LA 70148, USA.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):891-3. doi: 10.1016/j.bmcl.2008.11.110. Epub 2008 Dec 6.
Abstract
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 (K(i)=11 nM) exhibited the most potent affinity of the series.
摘要
一系列 4-烷氧基羰基-1,5-二芳基-1,2,3-三唑通过点击化学被区域选择性地合成，并在 CB1 大麻素受体上进行了评估。正丙酯 11（K(i)=4.6 nM）和苯基酯 14（K(i)=11 nM）表现出该系列中最强的亲和力。
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