Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Bastian, Frehland"'
Publikováno v:
Acta Crystallographica Section E: Crystallographic Communications, Vol 72, Iss 5, Pp 683-686 (2016)
In the title compound, C25H27NO4S, which crystallized as a racemate, the relative configuration of the adjacent OH and CH3 groups on the azepine ring is trans. The seven-membered azepin ring has a chair-like conformation. The planar aromatic rings of
Externí odkaz:
https://doaj.org/article/1d63753fb1994846bc101198fce474fa
Publikováno v:
Acta Crystallographica Section E: Crystallographic Communications, Vol 72, Iss 5, Pp 687-691 (2016)
The title compounds, C22H29NO2 (3) and C22H29NO2 (4) [systematic names: (1S*,2R*)-7-methoxy-2-methyl-3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol and (1R*,2R*)-7-methoxy-2-methyl-3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ol,
Externí odkaz:
https://doaj.org/article/8fd1fbe1514a413e81dec9feabf6f59c
Autor:
Kirstin Lehmkuhl, Patrizia Diana, Hendrik Jonas, Jens Köhler, Dirk Schepmann, Daniele Aiello, Bernhard Wünsch, Bastian Frehland
Conformationally restricted bicyclic KOR agonists 10 with an endo configured amino moiety were synthesized to analyze the bioactive conformation of conformationally flexible KOR agonists such as 2-5. A seven-step, chiral pool synthesis starting with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eaea984e7f93d339c717b4dac4c9a226
http://hdl.handle.net/10447/521671
http://hdl.handle.net/10447/521671
Autor:
Hendrik, Jonas, Daniele, Aiello, Bastian, Frehland, Kirstin, Lehmkuhl, Dirk, Schepmann, Jens, Köhler, Patrizia, Diana, Bernhard, Wünsch
Publikováno v:
Organicbiomolecular chemistry. 19(38)
Conformationally restricted bicyclic KOR agonists 10 with an
Autor:
Maia Datunashvili, Michael Hollmann, Simone Thum, Julian A. Schreiber, Bernhard Wünsch, Guiscard Seebohm, Dirk Schepmann, Bastian Frehland, Thomas Budde, Nathalie Strutz-Seebohm
Publikováno v:
Communications Biology, Vol 2, Iss 1, Pp 1-14 (2019)
N-methyl-D-aspartate receptors (NMDARs), especially GluN2B-containing NMDARs, are associated with neurodegenerative diseases like Parkinson, Alzheimer and Huntington based on their high Ca2+ conductivity. Overactivation leads to high intracellular Ca
Autor:
Alexander Markus, Julian A. Schreiber, Gunnar Goerges, Bastian Frehland, Dirk Schepmann, Constantin Daniliuc, Roland Fröhlich, Guiscard Seebohm, Bernhard Wünsch
Publikováno v:
Archiv der Pharmazie. 355:2200225
Negative allosteric modulators of N-methyl- d-aspartate receptors containing the GluN2B subunit represent promising drug candidates for the treatment of various neurological disorders including stroke, epilepsy, and Parkinson's disease. To increase t
Autor:
Dirk Schepmann, Elena Bechthold, Guiscard Seebohm, Cristina García, Freddy A. Bernal, Kirstin Lehmkuhl, Constantin G. Daniliuc, Bastian Frehland, Julian A. Schreiber, Thomas J. Schmidt, Bernhard Wünsch, Inés Alvarez
Publikováno v:
Journal of Medicinal Chemistry
Ifenprodil (1) is a potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonist that is used as a cerebral vasodilator and has been examined in clinical trials for the treatment of drug addiction, idiopathic pulmonary fibrosis, and COVID-
Publikováno v:
Archiv der Pharmazie. 355:2200177
Inspired by besonprodil, the phenol of potent negative allosteric modulators of GluN2B-N-methyl-d-aspartate (NMDA) receptors was replaced by a benzoxazolone system. To increase the similarity to the lead compounds, an additional methyl moiety was ins
Autor:
Alexander Markus, Julian A. Schreiber, Gunnar Goerges, Bastian Frehland, Guiscard Seebohm, Dirk Schepmann, Bernhard Wünsch
Publikováno v:
Archiv der Pharmazie. 355:2200147
Tricyclic tetrahydrooxazolo[4,5-h]-[3]benzazepin-9-ols 22 were designed as phenol bioisosteres of tetrahydro-3-benzazepine-1,7-diols. Key features of the synthesis are the introduction of the trifluoromethylsulfonyl and allyl protective groups at the
Publikováno v:
ChemMedChem. 13:446-452
Because only a few studies have investigated the affinity and functional activity of NMDA receptor open channel blockers under the same assay conditions, a comparative study of common open channel blockers is of major interest. The pharmacological ac