- Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors
-
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. 2009 American Chemical Society.
- Kapanda, Coco N.,Muccioli, Giulio G.,Labar, Geoffray,Poupaert, Jacques H.,Lambert, Didier M.
-
experimental part
p. 7310 - 7314
(2010/07/14)
-
- Synthesis characterization and biological evaluation of 2-methyl-3-(N-substituted thiocarbamoylthio)acetamido-4(3H)-quinazolinones
-
Reaction of 3-chloroacetamido-2-methyl-4(3H)-quinazolinones (1 and 2) with appropriately substituted potassium dithiocarbamates (3) furnished 2-methyl-3-(N-substituted thiocarbamoylthio)acetamido-4(3H)-quinazolinones (4 and 5) which exist as isomeric mixtures. The structures of 4 and 5 were determined by analytical and spectral (IR, 1H-NMR, EIMS, CIMS(CH4 or NH3)) methods. All the compounds except for 4g and 5g were tested for antimicrobial activity against some bacteria und fungi. Only 4b and 4c were found active against Staphylococcus aureus (MIC 100 μg/ml). 4d, 4e, 4g, 4h, 5a-f and 5h were also evaluated for anticonvulsant activity but were found inactive.
- Capan,Ergenc,Buyuktimkin,Yulug
-
p. 243 - 250
(2007/10/02)
-