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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: guba w. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
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: guba w. 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
G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a survey.
Kratochwil NA, Gatti-McArthur S, Hoener MC, Lindemann L, Christ AD, Green LG, Guba W, Martin RE, Malherbe P, Porter RH, Slack JP, Winnig M, Dehmlow H, Grether U, Hertel C, Narquizian R, Panousis CG, Kolczewski S, Steward L. Kratochwil NA, et al. Among authors: guba w. Curr Top Med Chem. 2011;11(15):1902-24. doi: 10.2174/156802611796391267. Curr Top Med Chem. 2011. PMID: 21470172
A Real-World Perspective on Molecular Design.
Kuhn B, Guba W, Hert J, Banner D, Bissantz C, Ceccarelli S, Haap W, Körner M, Kuglstatter A, Lerner C, Mattei P, Neidhart W, Pinard E, Rudolph MG, Schulz-Gasch T, Woltering T, Stahl M. Kuhn B, et al. Among authors: guba w. J Med Chem. 2016 May 12;59(9):4087-102. doi: 10.1021/acs.jmedchem.5b01875. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878596
Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.
Alig L, Alsenz J, Andjelkovic M, Bendels S, Bénardeau A, Bleicher K, Bourson A, David-Pierson P, Guba W, Hildbrand S, Kube D, Lübbers T, Mayweg AV, Narquizian R, Neidhart W, Nettekoven M, Plancher JM, Rocha C, Rogers-Evans M, Röver S, Schneider G, Taylor S, Waldmeier P. Alig L, et al. Among authors: guba w. J Med Chem. 2008 Apr 10;51(7):2115-27. doi: 10.1021/jm701487t. Epub 2008 Mar 13. J Med Chem. 2008. PMID: 18335976
Structure-Activity Relationship Studies of Pyridine-Based Ligands and Identification of a Fluorinated Derivative for Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors.
Haider A, Kretz J, Gobbi L, Ahmed H, Atz K, Bürkler M, Bartelmus C, Fingerle J, Guba W, Ullmer C, Honer M, Knuesel I, Weber M, Brink A, Herde AM, Keller C, Schibli R, Mu L, Grether U, Ametamey SM. Haider A, et al. Among authors: guba w. J Med Chem. 2019 Dec 26;62(24):11165-11181. doi: 10.1021/acs.jmedchem.9b01280. Epub 2019 Dec 5. J Med Chem. 2019. PMID: 31751140
6-Alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds.
Röver S, Andjelkovic M, Bénardeau A, Chaput E, Guba W, Hebeisen P, Mohr S, Nettekoven M, Obst U, Richter WF, Ullmer C, Waldmeier P, Wright MB. Röver S, et al. Among authors: guba w. J Med Chem. 2013 Dec 27;56(24):9874-96. doi: 10.1021/jm4010708. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24175572
Can we discover pharmacological promiscuity early in the drug discovery process?
Peters JU, Hert J, Bissantz C, Hillebrecht A, Gerebtzoff G, Bendels S, Tillier F, Migeon J, Fischer H, Guba W, Kansy M. Peters JU, et al. Among authors: guba w. Drug Discov Today. 2012 Apr;17(7-8):325-35. doi: 10.1016/j.drudis.2012.01.001. Epub 2012 Jan 16. Drug Discov Today. 2012. PMID: 22269136 Review.
β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D, Muser T, Schnider C, Jacobsen H, Ozmen L, Bergadano A, Banner DW, Hochstrasser R, Kuglstatter A, David-Pierson P, Fischer H, Polara A, Narquizian R. Hilpert H, et al. Among authors: guba w. J Med Chem. 2013 May 23;56(10):3980-95. doi: 10.1021/jm400225m. Epub 2013 May 2. J Med Chem. 2013. PMID: 23590342
53 results