Journal
MOLECULES
Volume 26, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/molecules26113296
Keywords
monoacylglycerol lipase; fatty acid amide hydrolase; disulfiram
Funding
- King Abdulaziz City for Science and Technology (KACST) [2-17-03-007-0010]
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Novel disulfiram derivatives were evaluated as potent inhibitors of MAGL, showing high selectivity over FAAH. Compound 2i displayed low micromolar inhibition of MAGL without inhibitory activity against FAAH.
Monoacylglycerol lipase (MAGL) is a key enzyme in the human endocannabinoid system. It is also the main enzyme responsible for the conversion of 2-arachidonoyl glycerol (2-AG) to arachidonic acid (AA), a precursor of prostaglandin synthesis. The inhibition of MAGL activity would be beneficial for the treatment of a wide range of diseases, such as inflammation, neurodegeneration, metabolic disorders and cancer. Here, the author reports the pharmacological evaluation of new disulfiram derivatives as potent inhibitors of MAGL. These analogues displayed high inhibition selectivity over fatty acid amide hydrolase (FAAH), another endocannabinoid-hydrolyzing enzyme. In particular, compound 2i inhibited MAGL in the low micromolar range. However, it did not show any inhibitory activity against FAAH.
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