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

详细信息    查看全文

• 作者：Jamal El Bakali ; Pauline Gilleron ; Mathilde Body-Malapel ; Roxane Mansouri ; Giulio G. Muccioli ; Madjid Djouina ; Am茅lie Barczyk ; Fr茅d茅rique Klupsch ; Virginie Andrzejak ; Emmanuelle Lipka ; Christophe Furman ; Didier M. Lambert ; Philippe Chavatte ; Pierre Desreumaux ; R茅gis Millet
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：October 25, 2012
• 年：2012
• 卷：55
• 期：20
• 页码：8948-8952
• 全文大小：304K
• 年卷期：v.55,no.20(October 25, 2012)
• ISSN：1520-4804

文摘

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.