| Title : 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors - Granchi_2016_J.Enzyme.Inhib.Med.Chem_31_137 |
| Author(s) : Granchi C , Rizzolio F , Bordoni V , Caligiuri I , Manera C , Macchia M , Minutolo F , Martinelli A , Giordano A , Tuccinardi T |
| Ref : J Enzyme Inhib Med Chem , 31 :137 , 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 microM, respectively). Furthermore, the best compound behaved as a reversible ligand and showed promising antiproliferative activity in cancer cells. |
| PubMedSearch : Granchi_2016_J.Enzyme.Inhib.Med.Chem_31_137 |
| PubMedID: 25669350 |
Granchi C, Rizzolio F, Bordoni V, Caligiuri I, Manera C, Macchia M, Minutolo F, Martinelli A, Giordano A, Tuccinardi T (2016)
4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors
J Enzyme Inhib Med Chem
31 :137
Granchi C, Rizzolio F, Bordoni V, Caligiuri I, Manera C, Macchia M, Minutolo F, Martinelli A, Giordano A, Tuccinardi T (2016)
J Enzyme Inhib Med Chem
31 :137