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.
|Autori:||Granchi, Carlotta; Rizzolio, F; Bordoni, Vittorio; Caligiuri, I; Manera, Clementina; Macchia, Marco; Minutolo, Filippo; Martinelli, Adriano; Giordano, A; Tuccinardi, Tiziano|
|Titolo:||4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors|
|Anno del prodotto:||2016|
|Digital Object Identifier (DOI):||10.3109/14756366.2015.1010530|
|Appare nelle tipologie:||1.1 Articolo in rivista|