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Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L. Jaeschke G, et al. Among authors: peters ju. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Aminomethylpyridines as DPP-IV inhibitors.
Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Zimmerli D, Boehringer M, Steger M, Loeffler BM. Peters JU, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3579-80. doi: 10.1016/j.bmcl.2004.04.049. Bioorg Med Chem Lett. 2004. PMID: 15177478
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Porter RH, Jaeschke G, Spooren W, Ballard TM, Büttelmann B, Kolczewski S, Peters JU, Prinssen E, Wichmann J, Vieira E, Mühlemann A, Gatti S, Mutel V, Malherbe P. Porter RH, et al. Among authors: peters ju. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. doi: 10.1124/jpet.105.089839. Epub 2005 Jul 22. J Pharmacol Exp Ther. 2005. PMID: 16040814
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
Büttelmann B, Peters JU, Ceccarelli S, Kolczewski S, Vieira E, Prinssen EP, Spooren W, Schuler F, Huwyler J, Porter RH, Jaeschke G. Büttelmann B, et al. Among authors: peters ju. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. doi: 10.1016/j.bmcl.2005.12.088. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439120
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Ceccarelli SM, Jaeschke G, Buettelmann B, Huwyler J, Kolczewski S, Peters JU, Prinssen E, Porter R, Spooren W, Vieira E. Ceccarelli SM, et al. Among authors: peters ju. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6. doi: 10.1016/j.bmcl.2006.12.006. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17189691
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Jaeschke G, Porter R, Büttelmann B, Ceccarelli SM, Guba W, Kuhn B, Kolczewski S, Huwyler J, Mutel V, Peters JU, Ballard T, Prinssen E, Vieira E, Wichmann J, Spooren W. Jaeschke G, et al. Among authors: peters ju. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1307-11. doi: 10.1016/j.bmcl.2006.12.033. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17196387
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Lübbers T, Böhringer M, Gobbi L, Hennig M, Hunziker D, Kuhn B, Löffler B, Mattei P, Narquizian R, Peters JU, Ruff Y, Wessel HP, Wyss P. Lübbers T, et al. Among authors: peters ju. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2966-70. doi: 10.1016/j.bmcl.2007.03.072. Epub 2007 Mar 25. Bioorg Med Chem Lett. 2007. PMID: 17418568
Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series.
Ceccarelli SM, Schlotterbeck G, Boissin P, Binder M, Buettelmann B, Hanlon S, Jaeschke G, Kolczewski S, Kupfer E, Peters JU, Porter RH, Prinssen EP, Rueher M, Ruf I, Spooren W, Stämpfli A, Vieira E. Ceccarelli SM, et al. Among authors: peters ju. ChemMedChem. 2008 Jan;3(1):136-44. doi: 10.1002/cmdc.200700203. ChemMedChem. 2008. PMID: 17994660
24 results