Abstract
This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibitors. A 69-fold selectivity against MAGL over FAAH was achieved for compound 16b (MAGL and FAAH IC50 = 1.6 and 111 μM, respectively). Furthermore, the best compound behaved as a reversible ligand and showed promising antiproliferative activity in cancer cells.
Original language | English |
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Pages (from-to) | 137-146 |
Number of pages | 10 |
Journal | Journal of Enzyme Inhibition and Medicinal Chemistry |
Volume | 31 |
Issue number | 1 |
DOIs | |
Publication status | Published - Jan 2 2016 |
Keywords
- Hydrolase
- MAGL
- MAGL inhibitors
- monoacylglycerol lipase
- monoacylglycerol lipase inhibitors
ASJC Scopus subject areas
- Drug Discovery
- Pharmacology