Document Report Card

ID: ALA1154683

Journal: J Med Chem

Title: Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.

Authors: Kapanda CN, Muccioli GG, Labar G, Poupaert JH, Lambert DM.

Abstract: Monoglyceride lipase (MGL) inhibition may offer an approach in treating diseases in which higher 2-arachidonoyglycerol activity would be beneficial. We report here the synthesis and pharmacological evaluation of bis(dialkylaminethiocarbonyl)disulfide derivatives as irreversible MGL inhibitors. Inhibition occurs through interactions with MGL C208 and C242 residues, and these derivatives exhibit high inhibition selectivity over fatty acid amide hydrolase, another endocannabinoid-hydrolyzing enzyme.

CiteXplore: 19883085

DOI: 10.1021/jm901323s