Structure–activity relationship of a new Series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors

…, A Romero, S Ortega-Gutiérrez, CJ Fowler…

Index: Cisneros, Jose A.; Bjoerklund, Emmelie; Gonzalez-Gil, Ines; Hu, Yanling; Canales, Angeles; Medrano, Francisco J.; Romero, Antonio; Ortega-Gutierrez, Silvia; Fowler, Christopher J.; Lopez-Rodriguez, Maria L. Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 824 - 836

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Citation Number: 11

Abstract

The two endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), play independent and nonredundant roles in the body. This makes the development of both selective and dual inhibitors of their inactivation an important priority. In this work we report a new series of inhibitors of monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH). Among them,(±)-oxiran-2-ylmethyl 6-(1, 1′-biphenyl-4-yl) hexanoate (8) and (2 ...