1. J Med Chem. 2009 Nov 26;52(22):7310-7314.

Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride
Lipase Inhibitors.

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

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.

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 [PubMed - as supplied by publisher]