Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Jens-Uwe Peters"'
Publikováno v:
CHIMIA, Vol 77, Iss 7/8 (2023)
Successful structure-based drug design (SBDD) requires the optimization of interactions with the target protein and the minimization of ligand strain. Both factors are often modulated by small changes in the chemical structure which can lead to profo
Externí odkaz:
https://doaj.org/article/5a77acfa0fab4271b95d75928bcd2ac6
Publikováno v:
CHIMIA, Vol 58, Iss 9 (2004)
Lead generation and the associated hit-to-lead process are key strategic elements in modern pharmaceutical research, and most companies have implemented this concept. Efficient lead generation is one of the main attempts to reduce the high attrition
Externí odkaz:
https://doaj.org/article/b7b5ff7cd95b44039ad8046baf2e7c8d
Autor:
Christian Lerner, Jens-Uwe Peters, Sonia Roberts, Susanne Mohr, Bernhard Fasching, Manfred Kansy, Hans Richter, Wolfgang Guba, Fabien Tillier, Jacques Migeon, Caterina Bissantz, Grégori Gerebtzoff, Rene Wyler, Christian Kramer, Stefanie Bendels
Publikováno v:
Journal of pharmacological and toxicological methods. 99
Background Several factors contribute to the development failure of novel pharmaceuticals, one of the most important being adverse effects in pre-clinical and clinical studies. Early identification of off-target compound activity can reduce safety-re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13c992581d78f6546595e988cab0fd94
https://pubmed.ncbi.nlm.nih.gov/31284073
https://pubmed.ncbi.nlm.nih.gov/31284073
Autor:
Georg Jaeschke, Urs Niederhauser, Beatrice David, Eric Vieira, Will Spooren, Martin Kuratli, Jens-Uwe Peters, Michael Honer, Wolfgang Guba, Thomas Hartung, Daniel Tännler, Christoph Funk, Nadia Bitter-Stoll, Porter Richard Hugh Phillip, Bernd Büttelmann, Daniel Rueher, Paul Spurr, Jörg Huwyler, Nicole Clemann, Eric Prinssen, Joseph G. Wettstein, Axel Pähler, Simona M. Ceccarelli, Patrick Boissin, Theodor Stoll, Antonio Ricci, Jürgen Wichmann, Ann Petersen, Manfred Schneider, Marianne Rueher, Edilio Borroni, Sabine Kolczewski, Anthony Harrison, Lothar Lindemann
Publikováno v:
Journal of Medicinal Chemistry. 58:1358-1371
Negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu5) have potential for the treatment of psychiatric diseases including depression, fragile X syndrome (FXS), anxiety, obsessive-compulsive disorders, and levodopa induced
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f629d43eba9d48337f793d5244811596
https://doi.org/10.1021/jm501642c
https://doi.org/10.1021/jm501642c
Publikováno v:
Tetrahedron Letters. 52:749-752
Several drugs (clozapine, chlorpromazine, imipramine, buspirone, diltiazem, and propranolol) were subjected to modified Udenfriend conditions (Fe 2+ /Mn 2+ /EDTA/ascorbic acid/O 2 ). From each reaction, one to four oxidation products were obtained in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8db9d25e14d47319408794bcb4a59ad2
https://doi.org/10.1016/j.tetlet.2010.12.014
https://doi.org/10.1016/j.tetlet.2010.12.014
Autor:
Torsten Hoffmann, Jens-Uwe Peters, Sleight Andrew, Heinz Stadler, André Alker, Lucinda Steward, Theresa M. Ballard, Will Spooren, Andreas Koblet, Schnider Patrick, Sonia Poli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3405-3408
During a program directed at selective NK(1) receptor antagonists, we serendipitously discovered an NK(1) receptor ligand with additional affinity for the NK(3) receptor. Recognising an opportunity for a drug discovery program aiming for dual NK(1)/N
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a4073de1fc025a68df92bf24e7f8c70
https://doi.org/10.1016/j.bmcl.2010.04.008
https://doi.org/10.1016/j.bmcl.2010.04.008
Publikováno v:
Tetrahedron Letters. 49:4029-4032
2-Quinolones are prepared from o -aminophenylketones by N-acylation with phosphonoalkanoylchlorides, followed by an intramolecular Horner–Wadsworth–Emmons olefination. The transformation proceeds under mild conditions, is generally applicable, gi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9a44d9c1b36f880522c94766d015faa1
https://doi.org/10.1016/j.tetlet.2008.04.088
https://doi.org/10.1016/j.tetlet.2008.04.088
Autor:
Martin Binder, Will Spooren, Simona M. Ceccarelli, Patrick Boissin, Steven P. Hanlon, Ernst Kupfer, Eric Prinssen, Andreas Stämpfli, Georg Jaeschke, Bernd Buettelmann, Iris Ruf, Jens-Uwe Peters, Eric Vieira, Sabine Kolczewski, Marianne Rueher, Porter Richard Hugh Phillip, Götz Schlotterbeck
Publikováno v:
ChemMedChem. 3:136-144
Detailed information on the metabolic fate of lead compounds can be a powerful tool for an informed approach to the stabilization of metabolically labile compounds in the lead optimization phase. The combination of high performance liquid chromatogra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c694b039de119ef8a1ee142de1820b2d
https://doi.org/10.1002/cmdc.200700203
https://doi.org/10.1002/cmdc.200700203
Autor:
Bernd Kuhn, Hans Peter Wessel, Jens-Uwe Peters, Patrizio Mattei, Robert Narquizian, Pierre C. Wyss, Luca Gobbi, Daniel Hunziker, Thomas Lübbers, Bernd Michael Löffler, Markus Bohringer, Yves Ruff, Michael Hennig
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2966-2970
In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits. Due to the difficult synthetic access to this compound class, 1,3-disubstituted 4-aminopiperidines were used as model compounds for optimi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cd6c90da848493eb8e57076b093f2bc
https://doi.org/10.1016/j.bmcl.2007.03.072
https://doi.org/10.1016/j.bmcl.2007.03.072
Autor:
Jens-Uwe Peters
Publikováno v:
Current Topics in Medicinal Chemistry. 7:579-595
Cyanopyrrolidines (cyanopyrrolidides, pyrrolidine-2-nitriles, prolinenitriles) as inhibitors of the serine protease dipeptidyl peptidase IV (DPP-IV, DP IV, CD26, EC 3.4.14.5) were first reported in 1995. The interest in this compound class grew immen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90bc183bc1b3ba642a8b6c6afa544d6f
https://doi.org/10.2174/156802607780091000
https://doi.org/10.2174/156802607780091000