| Literature DB >> 19883085 |
Coco N Kapanda1, Giulio G Muccioli, Geoffray Labar, Jacques H Poupaert, Didier M Lambert.
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.Entities:
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Year: 2009 PMID: 19883085 DOI: 10.1021/jm901323s
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446