3-Alkyl-(5,5′-diphenyl)imidazolidinediones as new cannabinoid receptor ligands

Twenty-four 3-alkyl-(5,5′-diphenyl)imidazolidinediones were synthesized and evaluated as new cannabinoid receptor ligands. Three compounds exhibited a Ki value around 100 nM against [ 3H]-SR 141716A binding obtained from human CB 1 transfected CHO cells membranes. The lack of change of affinity in t...

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Published inBioorganic & medicinal chemistry letters Vol. 9; no. 15; pp. 2233 - 2236
Main Authors Kanyonyo, Martial, Govaerts, Sophie J., Hermans, Emmanuel, Poupaert, Jacques H., Lambert, Didier M.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 02.08.1999
Elsevier
Subjects
Biological and medical sciences
Medical sciences
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Imidazole derivatives
Five membered ring
Structure activity relation
Nitrogen heterocycle
Benzenic compound
Bromine Organic compounds
Cannabinoid
Chemical synthesis
In vitro
Biological receptor
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Summary:Twenty-four 3-alkyl-(5,5′-diphenyl)imidazolidinediones were synthesized and evaluated as new cannabinoid receptor ligands. Three compounds exhibited a Ki value around 100 nM against [ 3H]-SR 141716A binding obtained from human CB 1 transfected CHO cells membranes. The lack of change of affinity in the presence of a non hydrolyzable GTP analogue seems to indicate they are cannabinoid antagonists. Twenty-four 3-alkyl-(5,5′-diphenyl)imidazolidinediones were prepared as new cannabinoid receptor ligands. Three compounds including 20 exhibited a Ki value around 100 nM against [ 3H]-SR 141716A binding obtained from human CB1 transfected CHO cells membranes.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00353-4