Synthesis and Pharmacological Evaluation of Chlorinated <Emphasis Type="Italic">N</Emphasis>-Alkyl-3- and -5-(2-hydroxyphenyl)pyrazoles as <Emphasis Type="Italic">CB</Emphasis><Subscript>1</Subscript> Cannabinoid Ligands期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Synthesis and Pharmacological Evaluation of Chlorinated N-Alkyl-3- and -5-(2-hydroxyphenyl)pyrazoles as CB1 Cannabinoid Ligands

Authors:	Vera L. M. Silva Artur M. S. Silva Diana C. G. A. Pinto Nadine Jagerovic Luis F. Callado José A. S. Cavaleiro José Elguero

Affiliation:	(1) Chemistry Department, University of Aveiro, Aveiro, Portugal;(2) Instituto de Química Médica (CSIC), Madrid, Spain;(3) Pharmacology Department, University of the Basque Country (UPV/EHU), Bizkaia, Spain

Abstract:	Summary. The syntheses of several new 3- and 5-(4-chloro-2-hydroxyphenyl)-5- and -3-(2,4-dichlorophenyl)-1-alkylpyrazoles are reported. These syntheses started from simple chlorophenols, 2,4-dichlorobenzaldehyde or ethyl 2,4-dichlorobenzoate in order to prepare pyrazoles bearing three and four chloro substituents in certain positions. The affinity of these compounds towards the CB ₁ type cannabinoids receptors was then evaluated in human brain tissues (frontal cortex). The results showed that some of the compounds exhibit affinity towards this kind of receptors in the micromolar range.

Keywords:	. 3- and 5-(2-Hydroxyphenyl)-N-alkylpyrazoles Chloropyrazoles NMR spectroscopy CB ₁ cannabinoid receptors Radioligand.
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