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J Med Chem. 2012 Oct 25;55(20):8948-52. doi: 10.1021/jm3008568. Epub 2012 Oct 12.

4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis.

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ICPAL, Université Lille Nord de France , EA4481, IFR114, 3 Rue du Pr. Laguesse, BP 83, F-59006 Lille Cedex, France.


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.

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