Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors

N Matuszak, GG Muccioli, G Labar…

文献索引：Matuszak, Nicolas; Muccioli, Giulio G.; Labar, Geoffray; Lambert, Didier M. Journal of Medicinal Chemistry, 2009 , vol. 52, # 23 p. 7410 - 7420

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被引用次数: 78

摘要

The endocannabinoid 2-arachidonoylglycerol (2-AG) plays a major role in many physiological processes, and its action is quickly terminated via enzymatic hydrolysis catalyzed by monoglyceride lipase (MGL). Regulating its endogenous level could offer therapeutic opportunities; however, few selective MGL inhibitors have been described so far. Here, we describe the synthesis of N-substituted maleimides and their pharmacological ...