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

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)7486-7490
Number of pages5
JournalJournal of Medicinal Chemistry
Volume48
Issue number23
DOIs
Publication statusPublished - 17 Nov 2005

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