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231 results

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Page 1
Structure-Guided Discovery of cis-Hexahydro-pyrido-oxazinones as Reversible, Drug-like Monoacylglycerol Lipase Inhibitors.
Kuhn B, Ritter M, Hornsperger B, Bell C, Kocer B, Rombach D, Lutz MDR, Gobbi L, Kuratli M, Bartelmus C, Bürkler M, Koller R, Tosatti P, Ruf I, Guerard M, Pavlovic A, Stephanus J, O'Hara F, Wetzl D, Saal W, Stihle M, Roth D, Hug M, Huber S, Heer D, Kroll C, Topp A, Schneider M, Gertsch J, Glasmacher S, van der Stelt M, Martella A, Wittwer MB, Collin L, Benz J, Richter H, Grether U. Kuhn B, et al. Among authors: gertsch j. J Med Chem. 2024 Oct 24;67(20):18448-18464. doi: 10.1021/acs.jmedchem.4c01769. Epub 2024 Oct 3. J Med Chem. 2024. PMID: 39360636
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M. Soethoudt M, et al. Among authors: gertsch j. Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958. Nat Commun. 2017. PMID: 28045021 Free PMC article.
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
Aghazadeh Tabrizi M, Baraldi PG, Baraldi S, Ruggiero E, De Stefano L, Rizzolio F, Di Cesare Mannelli L, Ghelardini C, Chicca A, Lapillo M, Gertsch J, Manera C, Macchia M, Martinelli A, Granchi C, Minutolo F, Tuccinardi T. Aghazadeh Tabrizi M, et al. Among authors: gertsch j. J Med Chem. 2018 Feb 8;61(3):1340-1354. doi: 10.1021/acs.jmedchem.7b01845. Epub 2018 Jan 22. J Med Chem. 2018. PMID: 29309142
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
Granchi C, Lapillo M, Glasmacher S, Bononi G, Licari C, Poli G, El Boustani M, Caligiuri I, Rizzolio F, Gertsch J, Macchia M, Minutolo F, Tuccinardi T, Chicca A. Granchi C, et al. Among authors: gertsch j. J Med Chem. 2019 Feb 28;62(4):1932-1958. doi: 10.1021/acs.jmedchem.8b01483. Epub 2019 Feb 11. J Med Chem. 2019. PMID: 30715876
Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.
Sarott RC, Westphal MV, Pfaff P, Korn C, Sykes DA, Gazzi T, Brennecke B, Atz K, Weise M, Mostinski Y, Hompluem P, Koers E, Miljuš T, Roth NJ, Asmelash H, Vong MC, Piovesan J, Guba W, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Benito-Cuesta I, Grande T, Ruiz de Martı N Esteban S, Yeliseev A, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Yuan CY, Drobyski WR, Saroz Y, Grimsey N, Honer M, Fingerle J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, McCormick PJ, Ullmer C, Oddi S, Maccarrone M, Veprintsev DB, Nazaré M, Grether U, Carreira EM. Sarott RC, et al. Among authors: gertsch j. J Am Chem Soc. 2020 Oct 7;142(40):16953-16964. doi: 10.1021/jacs.0c05587. Epub 2020 Sep 29. J Am Chem Soc. 2020. PMID: 32902974
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
Granchi C, Bononi G, Ferrisi R, Gori E, Mantini G, Glasmacher S, Poli G, Palazzolo S, Caligiuri I, Rizzolio F, Canzonieri V, Perin T, Gertsch J, Sodi A, Giovannetti E, Macchia M, Minutolo F, Tuccinardi T, Chicca A. Granchi C, et al. Among authors: gertsch j. Eur J Med Chem. 2021 Jan 1;209:112857. doi: 10.1016/j.ejmech.2020.112857. Epub 2020 Oct 7. Eur J Med Chem. 2021. PMID: 33045662
Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives.
Bononi G, Di Stefano M, Poli G, Ortore G, Meier P, Masetto F, Caligiuri I, Rizzolio F, Macchia M, Chicca A, Avan A, Giovannetti E, Vagaggini C, Brai A, Dreassi E, Valoti M, Minutolo F, Granchi C, Gertsch J, Tuccinardi T. Bononi G, et al. Among authors: gertsch j. J Med Chem. 2022 May 26;65(10):7118-7140. doi: 10.1021/acs.jmedchem.1c01806. Epub 2022 May 6. J Med Chem. 2022. PMID: 35522977 Free PMC article.
231 results