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.

4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors

GRANCHI, CARLOTTA;BORDONI, VITTORIO;MANERA, CLEMENTINA;MACCHIA, MARCO;MINUTOLO, FILIPPO;MARTINELLI, ADRIANO;TUCCINARDI, TIZIANO
2016

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.
Granchi, Carlotta; Rizzolio, F; Bordoni, Vittorio; Caligiuri, I; Manera, Clementina; Macchia, Marco; Minutolo, Filippo; Martinelli, Adriano; Giordano, A; Tuccinardi, Tiziano
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/659663
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