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
2016-01-01

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.
2016
Granchi, Carlotta; Rizzolio, F; Bordoni, Vittorio; Caligiuri, I; Manera, Clementina; Macchia, Marco; Minutolo, Filippo; Martinelli, Adriano; Giordano, A; Tuccinardi, Tiziano
File in questo prodotto:
File Dimensione Formato  
2016_1.pdf

solo utenti autorizzati

Descrizione: reprint
Tipologia: Versione finale editoriale
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 510.27 kB
Formato Adobe PDF
510.27 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
Tuccinardi.pdf

Open Access dal 01/04/2017

Tipologia: Documento in Post-print
Licenza: Tutti i diritti riservati (All rights reserved)
Dimensione 753.5 kB
Formato Adobe PDF
753.5 kB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/659663
Citazioni
  • ???jsp.display-item.citation.pmc??? 5
  • Scopus 23
  • ???jsp.display-item.citation.isi??? 19
social impact