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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 32, 2017 - Issue 1
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Research Paper

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

Carlotta GranchiDepartment of Pharmacy, University of Pisa, Pisa, Italy; ORCID Iconhttp://orcid.org/0000-0002-5849-0722View further author information
ORCID Icon,
Isabella CaligiuriUnit of Pathology, Department of Molecular Biology and Translational Research, National Cancer Institute and Center for Molecular Biomedicine, Aviano, Pordenone, Italy; View further author information
,
Eleonora BertelliDepartment of Pharmacy, University of Pisa, Pisa, Italy; View further author information
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Giulio PoliDepartment of Pharmacy, University of Pisa, Pisa, Italy; View further author information
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Flavio RizzolioDepartment of Molecular Sciences and Nanosystems, Ca’ Foscari Università di Venezia, Venezia-Mestre, Italy; View further author information
,
Marco MacchiaDepartment of Pharmacy, University of Pisa, Pisa, Italy; View further author information
,
Adriano MartinelliDepartment of Pharmacy, University of Pisa, Pisa, Italy; View further author information
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Filippo MinutoloDepartment of Pharmacy, University of Pisa, Pisa, Italy; ORCID Iconhttp://orcid.org/0000-0002-3312-104XView further author information
ORCID Icon &
Tiziano TuccinardiDepartment of Pharmacy, University of Pisa, Pisa, Italy; ;Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology, Temple University, Philadelphia, PA, USACorrespondence[email protected]
ORCID Iconhttp://orcid.org/0000-0002-6205-4069View further author information
ORCID Icon show all
Pages 1240-1252 | Received 28 Jul 2017, Accepted 23 Aug 2017, Published online: 22 Sep 2017

Citations (26)

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Giulio Poli, Margherita Lapillo, Vibhu Jha, Nayla Mouawad, Isabella Caligiuri, Marco Macchia, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi & Carlotta Granchi. (2019) Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 34:1, pages 589-596.
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Giulio Poli, Margherita Lapillo, Carlotta Granchi, Jessica Caciolla, Nayla Mouawad, Isabella Caligiuri, Flavio Rizzolio, Thierry Langer, Filippo Minutolo & Tiziano Tuccinardi. (2018) Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 33:1, pages 956-961.
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Carlotta Granchi, Isabella Caligiuri, Filippo Minutolo, Flavio Rizzolio & Tiziano Tuccinardi. (2017) A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017). Expert Opinion on Therapeutic Patents 27:12, pages 1341-1351.
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Articles from other publishers (23)

Abhishek Kashyap, Suresh Kumar & Rohit Dutt. (2022) A Review on Structurally Diversified Synthesized Molecules as Monoacylglycerol Lipase Inhibitors and their Therapeutic uses. Current Drug Research Reviews 14:2, pages 96-115.
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Muhammad Adeel, Gloria Saorin, Giacomo Boccalon, Andrea Augusto Sfriso, Salvatore Parisi, Isabella Moro, Stefano Palazzolo, Isabella Caligiuri, Carlotta Granchi, Giuseppe Corona, Maja Cemazar, Vincenzo Canzonieri, Tiziano Tuccinardi & Flavio Rizzolio. (2022) A carrier free delivery system of a monoacylglycerol lipase hydrophobic inhibitor. International Journal of Pharmaceutics 613, pages 121374.
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Ashraf N. Abdalla, Miriana Di Stefano, Giulio Poli, Tiziano Tuccinardi, Ammar Bader, Antonio Vassallo, Mohamed E. Abdallah, Mahmoud Zaki El-Readi, Bassem Refaat, Alanood S. Algarni, Rizwan Ahmad, Hamad M. Alkahtani, Alaa A.-M. Abdel-Aziz, Adel S. El-Azab & Aljawharah Alqathama. (2021) Co-Inhibition of P-gp and Hsp90 by an Isatin-Derived Compound Contributes to the Increase of the Chemosensitivity of MCF7/ADR-Resistant Cells to Doxorubicin. Molecules 27:1, pages 90.
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Giulia Bononi, Giacomo Tonarini, Giulio Poli, Ivana Barravecchia, Isabella Caligiuri, Marco Macchia, Flavio Rizzolio, Gian Carlo Demontis, Filippo Minutolo, Carlotta Granchi & Tiziano Tuccinardi. (2021) Monoacylglycerol lipase (MAGL) inhibitors based on a diphenylsulfide-benzoylpiperidine scaffold. European Journal of Medicinal Chemistry 223, pages 113679.
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Shivani Jaiswal & Senthil Raja Ayyannan. (2021) Anticancer Potential of Small‐Molecule Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase. ChemMedChem 16:14, pages 2172-2187.
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C. J. Fowler. (2021) The endocannabinoid system – current implications for drug development. Journal of Internal Medicine 290:1, pages 2-26.
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Francesco Balestri, Giulio Poli, Carlotta Pineschi, Roberta Moschini, Mario Cappiello, Umberto Mura, Tiziano Tuccinardi & Antonella Del Corso. (2020) Aldose Reductase Differential Inhibitors in Green Tea. Biomolecules 10:7, pages 1003.
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Bin Zhu, Peter J. Connolly, Yue-Mei Zhang, Mark E. McDonnell, Haiyan Bian, Shu-Chen Lin, Li Liu, Sui-Po Zhang, Kristen M. Chevalier, Michael R. Brandt, Cynthia M. Milligan, Christopher M. Flores & Mark J. Macielag. (2020) The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors. Bioorganic & Medicinal Chemistry Letters 30:14, pages 127243.
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Zhuoer Zhi, Wenting Zhang, Jingchun Yao, Yanguo Shang, Qingjing Hao, Zhong Liu, Yushan Ren, Jie Li, Guimin Zhang & Jinxin Wang. (2020) Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors. Journal of Medicinal Chemistry 63:11, pages 5783-5796.
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Giulio Poli & Tiziano Tuccinardi. (2020) Consensus Docking in Drug Discovery. Current Bioactive Compounds 16:3, pages 182-190.
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Bin Zhu, Peter J. Connolly, Sui-Po Zhang, Kristen M. Chevalier, Cynthia M. Milligan, Christopher M. Flores & Mark J. Macielag. (2020) The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL). Bioorganic & Medicinal Chemistry Letters 30:12, pages 127198.
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Angela Bisio, Anna M. Schito, Francesca Pedrelli, Ombeline Danton, Jakob K. Reinhardt, Giulio Poli, Tiziano Tuccinardi, Thomas Bürgi, Francesco De Riccardis, Mauro Giacomini, Daniela Calzia, Isabella Panfoli, Gian Carlo Schito, Matthias Hamburger & Nunziatina De Tommasi. (2020) Antibacterial and ATP Synthesis Modulating Compounds from Salvia tingitana . Journal of Natural Products 83:4, pages 1027-1042.
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Natasha L. Grimsey, Juha R. Savinainen, Bala Attili & Muneer Ahamed. (2020) Regulating membrane lipid levels at the synapse by small-molecule inhibitors of monoacylglycerol lipase: new developments in therapeutic and PET imaging applications. Drug Discovery Today 25:2, pages 330-343.
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Florian M. Dato, Jörg-Martin Neudörfl, Michael Gütschow, Bernd Goldfuss & Markus Pietsch. (2020) ω-Quinazolinonylalkyl aryl ureas as reversible inhibitors of monoacylglycerol lipase. Bioorganic Chemistry 94, pages 103352.
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Valentina Maggini, Marinella De Leo, Carlotta Granchi, Tiziano Tuccinardi, Alessio Mengoni, Eugenia Rosaria Gallo, Sauro Biffi, Renato Fani, Luisa Pistelli, Fabio Firenzuoli & Patrizia Bogani. (2019) The influence of Echinacea purpurea leaf microbiota on chicoric acid level. Scientific Reports 9:1.
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Sara Carpi, Egeria Scoditti, Marika Massaro, Beatrice Polini, Clementina Manera, Maria Digiacomo, Jasmine Esposito Salsano, Giulio Poli, Tiziano Tuccinardi, Stefano Doccini, Filippo Maria Santorelli, Maria Annunziata Carluccio, Marco Macchia, Martin Wabitsch, Raffaele De Caterina & Paola Nieri. (2019) The Extra-Virgin Olive Oil Polyphenols Oleocanthal and Oleacein Counteract Inflammation-Related Gene and miRNA Expression in Adipocytes by Attenuating NF-κB Activation. Nutrients 11:12, pages 2855.
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Tiziano Tuccinardi. (2019) Meet Our Editorial Board Member. Current Bioactive Compounds 15:2, pages 145-145.
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Carlotta Granchi, Margherita Lapillo, Sandra Glasmacher, Giulia Bononi, Cristina Licari, Giulio Poli, Maguie el Boustani, Isabella Caligiuri, Flavio Rizzolio, Jürg Gertsch, Marco Macchia, Filippo Minutolo, Tiziano Tuccinardi & Andrea Chicca. (2019) Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor. Journal of Medicinal Chemistry 62:4, pages 1932-1958.
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Ana Gil-Ordóñez, Mar Martín-Fontecha, Silvia Ortega-Gutiérrez & María L. López-Rodríguez. (2018) Monoacylglycerol lipase (MAGL) as a promising therapeutic target. Biochemical Pharmacology 157, pages 18-32.
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Marinella De Leo, Conny Guillen Huallpa, Britt Alvarado, Carlotta Granchi, Giulio Poli, Nunziatina De Tommasi & Alessandra Braca. (2018) New diterpenes from Salvia pseudorosmarinus and their activity as inhibitors of monoacylglycerol lipase (MAGL). Fitoterapia 130, pages 251-258.
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Giulia Bononi, Carlotta Granchi, Margherita Lapillo, Massimiliano Giannotti, Daniela Nieri, Serena Fortunato, Maguie El Boustani, Isabella Caligiuri, Giulio Poli, Kathryn E. Carlson, Sung Hoon Kim, Marco Macchia, Adriano Martinelli, Flavio Rizzolio, Andrea Chicca, John A. Katzenellenbogen, Filippo Minutolo & Tiziano Tuccinardi. (2018) Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors. European Journal of Medicinal Chemistry 157, pages 817-836.
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Ariel D. Quiroga & Richard Lehner. (2018) Pharmacological intervention of liver triacylglycerol lipolysis: The good, the bad and the ugly. Biochemical Pharmacology 155, pages 233-241.
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Elena Pini, Giulio Poli, Tiziano Tuccinardi, Laurent Chiarelli, Matteo Mori, Arianna Gelain, Luca Costantino, Stefania Villa, Fiorella Meneghetti & Daniela Barlocco. (2018) New Chromane-Based Derivatives as Inhibitors of Mycobacterium tuberculosis Salicylate Synthase (MbtI): Preliminary Biological Evaluation and Molecular Modeling Studies. Molecules 23:7, pages 1506.
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