Synthesis and SAR of 1,4,5,6-tetrahydropyridazines as potent cannabinoid CB1 receptor antagonists

被引：46

作者：

Lange, Jos H. M. ^{[1
]}

den Hartog, Arnold P. ^{[1
]}

van der Neut, Martina A. W. ^{[1
]}

van Vliet, Bernard J. ^{[1
]}

Kruse, Chris G. ^{[1
]}

机构：

[1] Solvay Pharmaceut, Chem Design & Synth Unit, Res Labs, NL-1381 CP Weesp, Netherlands

来源：

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

关键词：

Cannabinoid CB1; Antagonist; Inverse agonist; Scaffold hopping; Tetrahydropyridazine; MOLECULAR MODELING INVESTIGATIONS; ENDOCANNABINOID SYSTEM; BIOLOGICAL-PROPERTIES; INVERSE AGONISTS; LATEST ADVANCES; IMIDAZOLE; 3,4-DIARYLPYRAZOLINES; RECOGNITION; DERIVATIVES; INHIBITORS;

D O I：

10.1016/j.bmcl.2009.08.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and structure-activity relationship studies of 1,4,5,6-tetrahydropyridazines are described. The target compounds 3-5 represent a novel class of potent and selective CB1 receptor antagonists. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5675 / 5678

页数：4

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