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

High-throughput screening of the UCB sample collection identified the piperidinyl-sulfonyl benzoic ester 1 as a novel agonist for CB1 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.

Graphical abstractHigh-throughput screening identified the piperidinyl-sulfonyl benzoic ester 1 as a novel agonist for CB1 receptor with nanomolar affinity. We report here the pharmacological profile of compound 1 as well as preliminary biological activities in pain model. Analogs were purchased and the structure–affinity relationships among this novel class are discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide