Pyrazoles with a "click" 4-[N-(4-fluorobutyl)-1,2,3-triazole] substituent in position 3 are nanomolar CB1 receptor ligands

被引：6
|
作者：
Distinto, Rita [1 ,2 ]
Zanato, Chiara [1 ]
Montanari, Serena [1 ]
Cascio, Maria Grazia [1 ]
Lazzari, Paolo [2 ,3 ]
Pertwee, Roger [1 ]
Zanda, Matteo [1 ,4 ]
机构：
[1] Univ Aberdeen, Inst Med Sci, Kosterlitz Ctr Therapeut, Foresterhill AB25 2ZD, Scotland
[2] Neurosci PharmaNess Scarl, I-09010 Pula, CA, Italy
[3] KemoTech Srl, I-09010 Pula, CA, Italy
[4] CNR, ICRM, I-20131 Milan, Italy
来源：
JOURNAL OF FLUORINE CHEMISTRY | 2014年 / 167卷
关键词：
Cannabinoids; PET imaging; Fluorine; Sonogashira reaction; Click" chemistry; IN-VIVO; CANNABINOID RECEPTORS; ANTAGONIST; POTENT; BINDS; RADIOLIGAND; DERIVATIVES; SR141716A;
D O I：
10.1016/j.jfluchem.2014.07.010
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
Replacement of the 3-carbonylaminopiperidine substitutent with a "click" 4-[N-(4-fluorobutyl)-(1,2,3-triazolyl)] group in Rimonabant-type pyrazoles produced a novel class of nanomolar CB1 receptor ligands. Molecule 1d is the most promising lead with a K-i=23 nM for CB1, which is very close to that displayed by Rimonabant (SR141716), and fairly good CB1/CB2 selectivity (K-i CB2/K-i CB1 = 35.5), thus representing a promising candidate for [F-18]radiolabeling and PET Imaging studies of the CB1 receptor. (C) 2014 Elsevier B.V. All rights reserved.
引用
收藏
页码：184 / 191
页数：8
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