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Bioorg Med Chem Lett. 2007 Jan 1;17(1):272-7. Epub 2006 Oct 5.

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

Author information

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

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.

PMID:
17027269
DOI:
10.1016/j.bmcl.2006.09.049
[Indexed for MEDLINE]

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