Literature DB >> 25669350

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

Carlotta Granchi1, Flavio Rizzolio2, Vittorio Bordoni1, Isabella Caligiuri2, Clementina Manera1, Marco Macchia1, Filippo Minutolo1, Adriano Martinelli1, Antonio Giordano2, Tiziano Tuccinardi1,2.   

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 IC(50) = 1.6 and 111 µM, respectively). Furthermore, the best compound behaved as a reversible ligand and showed promising antiproliferative activity in cancer cells.

Entities:  

Keywords:  Hydrolase; MAGL; MAGL inhibitors; monoacylglycerol lipase; monoacylglycerol lipase inhibitors

Mesh：

Substances：

Year:  2015        PMID： 25669350     DOI： 10.3109/14756366.2015.1010530

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN： 1475-6366            Impact factor:   5.051


  5 in total

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Journal:  Nanoscale Adv       Date:  2021-07-08

2.  Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors.

Authors:  Carlotta Granchi; Isabella Caligiuri; Eleonora Bertelli; Giulio Poli; Flavio Rizzolio; Marco Macchia; Adriano Martinelli; Filippo Minutolo; Tiziano Tuccinardi
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

Review 3.  Polymer-Mediated Delivery of siRNAs to Hepatocellular Carcinoma: Variables Affecting Specificity and Effectiveness.

Authors:  Rossella Farra; Francesco Musiani; Francesca Perrone; Maja Čemažar; Urška Kamenšek; Federica Tonon; Michela Abrami; Aleš Ručigaj; Mario Grassi; Gabriele Pozzato; Deborah Bonazza; Fabrizio Zanconati; Giancarlo Forte; Maguie El Boustani; Lucia Scarabel; Marica Garziera; Concetta Russo Spena; Lucia De Stefano; Barbara Salis; Giuseppe Toffoli; Flavio Rizzolio; Gabriele Grassi; Barbara Dapas
Journal:  Molecules       Date:  2018-03-28       Impact factor: 4.411

4.  Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.

Authors:  Giulio Poli; Margherita Lapillo; Vibhu Jha; Nayla Mouawad; Isabella Caligiuri; Marco Macchia; Filippo Minutolo; Flavio Rizzolio; Tiziano Tuccinardi; Carlotta Granchi
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

Review 5.  Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy, neurological and metabolic disorders.

Authors:  Hui Deng; Weimin Li
Journal:  Acta Pharm Sin B       Date:  2019-10-18       Impact factor: 11.413
  5 in total

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