4‑Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands Part 2: Discovery of New Agonists Endowed with Protective Effect Against Experimental Colitis

Further on to our earlier work on 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 29 compounds, evaluated on both hCB1 and hCB2 cannabinoid receptors, and assessed 11 of them in the TNBS-induced...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Journal of medicinal chemistry 2012-10, Vol.55 (20), p.8948-8952
Hauptverfasser: El Bakali, Jamal, Gilleron, Pauline, Body-Malapel, Mathilde, Mansouri, Roxane, Muccioli, Giulio G, Djouina, Madjid, Barczyk, Amélie, Klupsch, Frédérique, Andrzejak, Virginie, Lipka, Emmanuelle, Furman, Christophe, Lambert, Didier M, Chavatte, Philippe, Desreumaux, Pierre, Millet, Régis
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Further on to our earlier work on 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 29 compounds, evaluated on both hCB1 and hCB2 cannabinoid receptors, and assessed 11 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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm3008568