Novel azoles as potent and selective cannabinoid CB2 receptor agonists

Jeremiah J Harnett; Christine Dolo; Isabelle Viossat; Florence Auger; Eric Ferrandis; Dennis Bigg; Michel Auguet; Serge Auvin; Pierre-E Chabrier

doi:10.1016/j.bmcl.2014.11.003

Novel azoles as potent and selective cannabinoid CB2 receptor agonists

Bioorg Med Chem Lett. 2015 Jan 1;25(1):88-91. doi: 10.1016/j.bmcl.2014.11.003. Epub 2014 Nov 7.

Authors

Jeremiah J Harnett¹, Christine Dolo, Isabelle Viossat, Florence Auger, Eric Ferrandis, Dennis Bigg, Michel Auguet, Serge Auvin, Pierre-E Chabrier

Affiliation

¹ Ipsen Innovation, Department of Compound Discovery, 5 Avenue du Canada, 91940 Les Ulis, France. jeremiah.harnett@ipsen.com

PMID: 25466197
DOI: 10.1016/j.bmcl.2014.11.003

Abstract

Novel azole compounds were prepared which demonstrated potent hCB2 binding activities with antioxidant activity for a selected compound. These compounds show good selectivity over the hCB1 receptor and are full agonists at the hCB2 receptor.

MeSH terms

Animals
Azoles / chemistry*
Azoles / metabolism*
CHO Cells
Cannabinoid Receptor Agonists / chemistry*
Cannabinoid Receptor Agonists / metabolism*
Cannabinoids / chemistry
Cannabinoids / metabolism
Cricetinae
Cricetulus
Humans
Receptor, Cannabinoid, CB2 / agonists*
Receptor, Cannabinoid, CB2 / metabolism*

Substances

Azoles
Cannabinoid Receptor Agonists
Cannabinoids
Receptor, Cannabinoid, CB2