178312-68-0Relevant academic research and scientific papers
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors
Bian, Haiyan,Brandt, Michael R.,Chevalier, Kristen M.,Connolly, Peter J.,Flores, Christopher M.,Lin, Shu-Chen,Liu, Li,Macielag, Mark J.,McDonnell, Mark E.,Milligan, Cynthia M.,Zhang, Sui-Po,Zhang, Yue-Mei,Zhu, Bin
, (2020/05/18)
Monoacylglycerol lipase (MAGL) is the enzyme that is primarily responsible for hydrolyzing the endocannabinoid 2-arachidononylglycerol (2-AG) to arachidonic acid (AA). It has emerged in recent years as a potential drug target for a number of diseases. Herein, we report the discovery of compound 6g from a series of azetidine-piperazine di-amide compounds as a potent, selective, and reversible inhibitor of MAGL. Oral administration of compound 6g increased 2-AG levels in rat brain and produced full efficacy in the rat complete Freund's adjuvant (CFA) model of inflammatory pain.
AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
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Page/Page column 79, (2010/11/05)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I), wherein Y, Z, R1, and s are defined herein.
