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.
|Titolo:||4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors|
|Autori interni:||RIZZOLIO, Flavio|
|Data di pubblicazione:||2016|
|Rivista:||JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY|
|Appare nelle tipologie:||2.1 Articolo su rivista |