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

Jos H M Lange; Arnold P den Hartog; Martina A W van der Neut; Bernard J van Vliet; Chris G Kruse

doi:10.1016/j.bmcl.2009.08.007

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

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5675-8. doi: 10.1016/j.bmcl.2009.08.007. Epub 2009 Aug 7.

Authors

Jos H M Lange¹, Arnold P den Hartog, Martina A W van der Neut, Bernard J van Vliet, Chris G Kruse

Affiliation

¹ Solvay Pharmaceuticals, Chemical Design and Synthesis Unit, Research Laboratories, C. J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands. jos.lange@solvay.com

PMID: 19699640
DOI: 10.1016/j.bmcl.2009.08.007

Abstract

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.

MeSH terms

Animals
CHO Cells
Cricetinae
Cricetulus
Humans
Pyridazines / chemical synthesis*
Pyridazines / chemistry
Pyridazines / pharmacology
Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
Receptor, Cannabinoid, CB1 / metabolism
Structure-Activity Relationship

Substances

Pyridazines
Receptor, Cannabinoid, CB1