Jamal El Bakali, Pauline Gilleron, Mathilde Body-Malapel, Roxane Mansouri, Giulio G Muccioli, Madjid Djouina, Amélie Barczyk, Frédérique Klupsch, Virginie Andrzejak, Emmanuelle Lipka, Christophe Furman, Didier M Lambert, Philippe Chavatte, Pierre Desreumaux, Régis Millet
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...
October 25, 2012: Journal of Medicinal Chemistry