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Optimizing TRPM4 inhibitors in the MHFP6 chemical space.
Delalande C, Awale M, Rubin M, Probst D, Ozhathil LC, Gertsch J, Abriel H, Reymond JL. Delalande C, et al. Among authors: gertsch j. Eur J Med Chem. 2019 Mar 15;166:167-177. doi: 10.1016/j.ejmech.2019.01.048. Epub 2019 Jan 24. Eur J Med Chem. 2019. PMID: 30708257
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
Bertini S, Chicca A, Gado F, Arena C, Nieri D, Digiacomo M, Saccomanni G, Zhao P, Abood ME, Macchia M, Gertsch J, Manera C. Bertini S, et al. Among authors: gertsch j. Bioorg Med Chem. 2017 Dec 15;25(24):6427-6434. doi: 10.1016/j.bmc.2017.10.015. Epub 2017 Oct 16. Bioorg Med Chem. 2017. PMID: 29079014 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
Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J, Lochner M, Peinelt C, Reymond JL, Abriel H. Ozhathil LC, et al. Among authors: gertsch j. Br J Pharmacol. 2018 Jun;175(12):2504-2519. doi: 10.1111/bph.14220. Epub 2018 Apr 29. Br J Pharmacol. 2018. PMID: 29579323 Free PMC article.
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
215 results