1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: New templates among the CB1 cannabinoid receptor inverse agonists

Giulio G. Muccioli, Johan Wouters, Gerhard K E Scriba, Wolfgang Poppitz, Jacques H. Poupaert, Didier M. Lambert

Résultats de recherche: Contribution à un journal/une revueArticle

Résumé

New 1-benzhydryl-3-phenylurea derivatives and their 1-benzhydryl-3- phenylthiourea isosteres were synthesized and evaluated for their human CB 1 and CB2 cannabinoid receptor affinity. These compounds proved to be selective CB1 cannabinoid receptor ligands, acting as inverse agonists in a [35S]-GTPγS assay. The affinity of 3,5,5′-triphenylimidazolidine-2,4-dione and 3,5,5′-triphenyl-2- thioxoimidazolidin-4-one derivatives, possessing the 1-benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea moiety, respectively, was also evaluated. In conclusion, the 1-benzhydryl-3-phenylurea scaffold seems to be a new interesting template of CB1 cannabinoid receptor inverse agonists.

langue originaleAnglais
Pages (de - à)7486-7490
Nombre de pages5
journalJournal of Medicinal Chemistry
Volume48
Numéro de publication23
Les DOIs
étatPublié - 17 nov. 2005

    Empreinte digitale

Contient cette citation