Abstract |
The CB2 cannabinoid receptor has been implicated in the regulation of intestinal inflammation. Following on from the promising activity of a series of 4-oxo-1,4-dihydroquinoline-3-carboxamide, we developed constrained analogues based on a 2H-pyrazolo[4,3-c]quinolin-3(5H)-one scaffold, with improved affinity for the hCB2 receptor and had very high selectivity over the hCB1 receptor. Importantly, the lead of this series (26, hCB2: K i = 0.39 nM, hCB1: K i > 3000 nM) was found to protect mice against experimental colitis after oral administration.
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Authors | Jamal El Bakali, Giulio G Muccioli, Mathilde Body-Malapel, Madjid Djouina, Frédérique Klupsch, Alina Ghinet, Amélie Barczyk, Nicolas Renault, Philippe Chavatte, Pierre Desreumaux, Didier M Lambert, Régis Millet |
Journal | ACS medicinal chemistry letters
(ACS Med Chem Lett)
Vol. 6
Issue 2
Pg. 198-203
(Feb 12 2015)
ISSN: 1948-5875 [Print] United States |
PMID | 25699149
(Publication Type: Journal Article)
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