1: J Med Chem. 2005 Nov 17;48(23):7486-90. 

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

Muccioli GG, Wouters J, Scriba GK, Poppitz W, Poupaert JH, Lambert DM.

Unite de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculte
de Medecine, Universite catholique de Louvain, Avenue E. Mounier 73, UCL-CMFA
7340, B-1200 Bruxelles, Belgium.

New 1-benzhydryl-3-phenylurea derivatives and their
1-benzhydryl-3-phenylthiourea isosteres were synthesized and evaluated for their
human CB1 and CB2 cannabinoid receptor affinity. These compounds proved to be
selective CB1 cannabinoid receptor ligands, acting as inverse agonists in a
[35S]-GTPgammaS 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.

PMID: 16279809 [PubMed - in process]