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J Med Chem. 2009 Nov 26;52(22):7310-4. doi: 10.1021/jm901323s.

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

Author information

1
Universite Catholique de Louvain, Louvain Drug Research Institute, Endocannabinoid and Cannabinoid Research Group, Drug Design and Discovery Center, Unite de Chimie Pharmaceutique et de Radiopharmacie, 73-40 Avenue E. Mounier UCL-CMFA (7340), B-1200 Bruxelles, Belgium.

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.

PMID:
19883085
DOI:
10.1021/jm901323s
[Indexed for MEDLINE]

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