The design, synthesis and biological evaluation of novel URB602 analogues as potential monoacylglycerol lipase inhibitors

…, M Agostino, DT Malone, E Yuriev, B Capuano

Index: Szabo, Monika; Agostino, Mark; Malone, Daniel T.; Yuriev, Elizabeth; Capuano, Ben Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 22 p. 6782 - 6787

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Citation Number: 9

Abstract

We have synthesised an extensive series of URB602 analogues as inhibitors of monoacylglycerol lipase (MAGL), which is the major enzyme responsible for metabolising the endocannabinoid 2-arachidonylglycerol. The recently identified crystal structure of MAGL was used in the design strategy and revealed three possible binding sites for URB602 and the proposed analogues. A test series of carbamate analogues were docked ...