1-Benzhydryl-3-phenylurea and 1-Benzhydryl-3-phenylthiourea Derivatives: New Templates among the CB sub(1) Cannabinoid Receptor Inverse Agonists

New 1-benzhydryl-3-phenylurea derivatives and their 1-benzhydryl-3-phenylthiourea isosteres were synthesized and evaluated for their human CB sub(1) and CB sub(2) cannabinoid receptor affinity. These compounds proved to be selective CB sub(1) cannabinoid receptor ligands, acting as inverse agonists...

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Published inJournal of medicinal chemistry Vol. 48; no. 23; pp. 7486 - 7490
Main Authors Muccioli, G G, Wouters, J, Scriba, GKE, Poppitz, W, Poupaert, J H, Lambert, D M
Format Journal Article
LanguageEnglish
Published 17.11.2005
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Summary:New 1-benzhydryl-3-phenylurea derivatives and their 1-benzhydryl-3-phenylthiourea isosteres were synthesized and evaluated for their human CB sub(1) and CB sub(2) cannabinoid receptor affinity. These compounds proved to be selective CB sub(1) cannabinoid receptor ligands, acting as inverse agonists in a [ super(35)S]-GTP gamma S 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 CB sub(1) cannabinoid receptor inverse agonists.
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ISSN:0022-2623
DOI:10.1021/jm0503906