Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies

N Lambeng; F Lebon; B Christophe; M Burton; M De Ryck; L Quéré

doi:10.1016/j.bmcl.2006.09.049

Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies

Bioorg Med Chem Lett. 2007 Jan 1;17(1):272-7. doi: 10.1016/j.bmcl.2006.09.049. Epub 2006 Oct 5.

Authors

N Lambeng¹, F Lebon, B Christophe, M Burton, M De Ryck, L Quéré

Affiliation

¹ CNS Molecular and Cellular Biology, Centre for CNS Innovation, UCB S.A., Chemin du Foriest, B-1420 Braine L'Alleud, Belgium.

PMID: 17027269
DOI: 10.1016/j.bmcl.2006.09.049

Abstract

High-throughput screening of the UCB sample collection identified the piperidinyl-sulfonyl benzoic ester 1 as a novel agonist for CB(1) receptor with nanomolar affinity. We report here the pharmacological profile of compound 1 as well as preliminary biological activities in pain model. Diverse close analogs of 1 were purchased and the structure-affinity relationships among this novel class are discussed.

MeSH terms

Analgesics / chemistry*
Analgesics / pharmacology*
Animals
Benzoates / chemistry*
Benzoates / pharmacology*
Humans
Ligands
Male
Mice
Mice, Inbred Strains
Receptor, Cannabinoid, CB1 / agonists*
Structure-Activity Relationship
Sulfonamides / chemistry*
Sulfonamides / pharmacology*

Substances

8-quinolinyl 4-methyl-3-(1-piperidinylsulfonyl)benzoate
Analgesics
Benzoates
Ligands
Receptor, Cannabinoid, CB1
Sulfonamides