Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Simone Thum"'
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:
Marta Pujol, Francisco R. Nieto, Eva Ayet, Bernhard Wünsch, Simone Thum, Simon M. Ametamey, Dirk Schepmann
Publikováno v:
European Journal of Medicinal Chemistry. 177:47-62
The class of tetrahydro-1H-3-benzazepines was systematically modified in 1-, 3- and 7-position. In particular, a F-atom was introduced in β- or γ-position of the 4-phenylbutyl side chain in 3-position. Ligands with the F-atom in γ-position possess
Autor:
Frederik Börgel, Inés Alvarez, Elisabeth Kronenberg, Melanie Bergkemper, Raquel F. Reinoso, Constantin G. Daniliuc, Dirk Schepmann, Bernhard Wünsch, Peter Brust, Simone Thum, Francisco R. Nieto
Publikováno v:
Journal of Medicinal Chemistry 61(2018), 9666-9690
In order to detect novel σ receptor ligands, the rigit spiro [[2]benzopyran-1,1'-cyclohexan]-4'-one was connected with amino moieties derived from σ2 receptor preferring lead compounds resulting in mixtures of trans- and cis-configured amines 6, 18
Autor:
Christina Weiss, Simone Thum, Anna Junker, Natalia V. Ortiz Zacarías, Artur K. Kokornaczyk, Henk de Vries, Masato Kitamura, Bernhard Wünsch, Laura H. Heitman, Michael Koch, Tomoaki Seki, Nuska Tschammer, Monica De Maria, Dirk Schepmann
Publikováno v:
European Journal of Medicinal Chemistry, 135, 401-413
Targeting CCR2 and CCR5 receptors is considered as promising concept for the development of novel antiinflammatory drugs. Herein, we present the development of the first probe-dependent positive allosteric modulator (PAM) of CCR5 receptors with a 2-b
Publikováno v:
Zeitschrift für Naturforschung B. 72:421-424
Chemokines (chemoattractant cytokines) together with their receptors represent key players in inflammatory processes. In order to develop novel chemokine CCR2 and CCR5 receptor antagonists, 2-benz-azepin-1-one 5 was prepared, which showed promising C
Publikováno v:
MedChemComm. 8:975-981
The influence of an F-atom in the side chain of benzo[7]annulen-7-amines on the affinity towards GluN2B subunit containing NMDA receptors and the selectivity over related receptors was investigated. The synthesis of 5a and 5b was performed by reducti
Autor:
Simone, Thum, Dirk, Schepmann, Eva, Ayet, Marta, Pujol, Francisco R, Nieto, Simon M, Ametamey, Bernhard, Wünsch
Publikováno v:
European journal of medicinal chemistry. 177
The class of tetrahydro-1H-3-benzazepines was systematically modified in 1-, 3- and 7-position. In particular, a F-atom was introduced in β- or γ-position of the 4-phenylbutyl side chain in 3-position. Ligands with the F-atom in γ-position possess
Autor:
Julian A, Schreiber, Dirk, Schepmann, Bastian, Frehland, Simone, Thum, Maia, Datunashvili, Thomas, Budde, Michael, Hollmann, Nathalie, Strutz-Seebohm, Bernhard, Wünsch, Guiscard, Seebohm
Publikováno v:
Communications Biology
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:
Raquel F. Reinoso, Simon M. Ametamey, Inés Alvarez, Bernhard Wünsch, Dirk Schepmann, Simone Thum
Publikováno v:
Journal of labelled compoundsradiopharmaceuticals. 62(8)
Because of their neuroprotective potential, GluN2B-selective ligands are of great interest for the treatment of various neurological and neurodegenerative disorders. Fluorinated benzo[7]annulen-7-amines, capable for PET, were synthesized by combining
Publikováno v:
ChemMedChem. 13(23)
The 4-benzylpiperidine moiety is a central structural element of potent N-methyl-d-aspartate (NMDA) receptor antagonists containing the GluN2B subunit. To obtain novel GluN2B ligands suitable for positron emission tomography, the benzylpiperidine moi