Document Detail


4-Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands Part 2: Discovery of New Agonists Endowed with Protective Effect Against Experimental Colitis.
MedLine Citation:
PMID:  23017078     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Further to our earlier work on a the 4-oxo-1,4-dihydropyridine, we describe herein our strategy to get access to potent selective CB2 receptor agonists. Thus, we designed and synthesized twenty nine compounds, evaluated on both hCB1 and hCB2 cannabinoid receptors and assessed eleven of them in the TNBS-induced colitis model in mice. Compound 48 was found to be the most efficient of our series, exhibiting an exquisite protection against experimental colitis, superior to the one observed after treatment with Pentasa.
Authors:
Jamal El Bakali; Pauline Gilleron; Mathilde Body-Malapel; Roxane Mansouri; Giulio G Muccioli; Madjid Djouina; Amélie Barczyk; Fréderique Klupsch; Virginie Andrzejak; Emanuelle Lipka; Christophe Furman; Didier M Lambert; Philippe Chavatte; Pierre Desreumaux; Regis Millet
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-28
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-9-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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