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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 31, 2016 - Issue 1
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Research Article

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

Carlotta GranchiDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Flavio RizzolioSbarro Institute for Cancer Research and Molecular Medicine Center for Biotechnology, Temple University, Philadelphia, PA, USA
,
Vittorio BordoniDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Isabella CaligiuriSbarro Institute for Cancer Research and Molecular Medicine Center for Biotechnology, Temple University, Philadelphia, PA, USA
,
Clementina ManeraDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Marco MacchiaDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Filippo MinutoloDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Adriano MartinelliDepartment of Pharmacy, University of Pisa, Pisa, Italy and
,
Antonio GiordanoSbarro Institute for Cancer Research and Molecular Medicine Center for Biotechnology, Temple University, Philadelphia, PA, USA
&
Tiziano TuccinardiDepartment of Pharmacy, University of Pisa, Pisa, Italy and ;Sbarro Institute for Cancer Research and Molecular Medicine Center for Biotechnology, Temple University, Philadelphia, PA, USACorrespondence[email protected]
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Pages 137-146 | Received 19 Dec 2014, Accepted 15 Jan 2015, Published online: 11 Feb 2015

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Amol U. Khandebharad, Pravin S. Kulkarni, Prakash S. Ubale, Bharat K. Dhotre, Prabhakar R. Kute & Swapnil R. Sarda. (2023) Synergism of Ultrasound and Choline Hydroxide for the Synthesis of the Azlactone Derivatives. Polycyclic Aromatic Compounds 43:4, pages 3546-3556.
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Giulia Bononi, Giulio Poli, Flavio Rizzolio, Tiziano Tuccinardi, Marco Macchia, Filippo Minutolo & Carlotta Granchi. (2021) An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present). Expert Opinion on Therapeutic Patents 31:2, pages 153-168.
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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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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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Carlotta Granchi, Isabella Caligiuri, Eleonora Bertelli, Giulio Poli, Flavio Rizzolio, Marco Macchia, Adriano Martinelli, Filippo Minutolo & Tiziano Tuccinardi. (2017) Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 32:1, pages 1240-1252.
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Articles from other publishers (16)

А. А. Оганесян, А. Т. Макичян, Е. Р. Алексанян & В. О. Топузян. (2022) Синтез 4-арилиден-2-арил-5(4H)-оксазолонов c применением системы Boc2o/пиридин. Chemical Journal of Armenia, pages 203-213.
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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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Samer Bayda, Emanuele Amadio, Simone Cailotto, Yahima Frión-Herrera, Alvise Perosa & Flavio Rizzolio. (2021) Carbon dots for cancer nanomedicine: a bright future. Nanoscale Advances 3:18, pages 5183-5221.
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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. Manera. (2021) Meet Our Editorial Board Member. Mini-Reviews in Medicinal Chemistry 21:6, pages 659-659.
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Xinjia Yan, Jing Wen, Lin Zhou, Lei Fan, Xiaobo Wang & Zhi Xu. (2020) Current Scenario of 1,3-oxazole Derivatives for Anticancer Activity. Current Topics in Medicinal Chemistry 20:21, pages 1916-1937.
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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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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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Hui Deng & Weimin Li. (2020) Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy, neurological and metabolic disorders. Acta Pharmaceutica Sinica B 10:4, pages 582-602.
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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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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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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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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. (2018) Polymer-Mediated Delivery of siRNAs to Hepatocellular Carcinoma: Variables Affecting Specificity and Effectiveness. Molecules 23:4, pages 777.
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Mojgan Aghazadeh Tabrizi, Pier Giovanni Baraldi, Stefania Baraldi, Emanuela Ruggiero, Lucia De Stefano, Flavio Rizzolio, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Andrea Chicca, Margherita Lapillo, Jürg Gertsch, Clementina Manera, Marco Macchia, Adriano Martinelli, Carlotta Granchi, Filippo Minutolo & Tiziano Tuccinardi. (2018) Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors. Journal of Medicinal Chemistry 61:3, pages 1340-1354.
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Carlotta Granchi, Flavio Rizzolio, Isabella Caligiuri, Marco Macchia, Adriano Martinelli, Filippo Minutolo & Tiziano Tuccinardi. 2018. Rational Drug Design. Rational Drug Design 335 346 .
Hamzeh Kiyani & Shiva Aslanpour. (2017) Synthesis of Erlenmeyer-Plöchl Azlactones Promoted by 5-Sulfosalicylic Acid. HETEROCYCLES 94:7, pages 1314.
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