Zobrazeno 1 - 10 of 16 pro vyhledávání: '"Georg Schlechtingen"'
1
Structural Design, Solid-Phase Synthesis and Activity of Membrane-Anchored β-Secretase Inhibitors on Aβ Generation from Wild-Type and Swedish-Mutant APP
Autor: Georg Schlechtingen, Margit Gruner, Hans-Joachim Knölker, Gary Jennings, Sebastian Weidlich, Heinke Schieb, Hans-Wolfgang Klafki, Jens Wiltfang, Philipp Linning
Publikováno v: Chemistry - A European Journal. 16:14412-14423
Covalent coupling of β-secretase inhibitors to a raftophilic lipid anchor via a suitable spacer by using solid-phase peptide synthesis leads to tripartite structures displaying substantially improved inhibition of cellular secretion of the β-amyloi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75909f9597938ab0a2db8fd3680c59f4
https://doi.org/10.1002/chem.201002878
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2
Transition Metals in Organic Synthesis, Part 82. First Total Synthesis of Methyl 6-Methoxycarbazole-3-carboxylate, Glycomaurrol, the Anti-TB Active Micromeline, and the Furo[2,3-c]carbazole Alkaloid Eustifoline-D
Autor: Georg Schlechtingen, Micha P. Krahl, Hans-Joachim Knölker, Tilo Krause, Ronny Forke
Publikováno v: Synlett. 2007:0268-0272
The palladium(0)-catalyzed amination followed by palladium(II)-catalyzed oxidative cyclization of the resulting diaryl-amine provides a short route to a series of 6-oxygenated carbazole alkaloids: glycozoline, 3-formyl-6-methoxycarbazole, methyl 6-me
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b7e3d615ac08c65396dd1ca2fc19b3b6
https://doi.org/10.1055/s-2007-967984
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3
Structure−Activity Relationships of Dynorphin A Analogues Modified in the Address Sequence
Autor: Joel A. Cassel, Georg Schlechtingen, Robert N. DeHaven, Murray Goodman, Joseph P. Taulane, Nga N. Chung, Jeffrey D. Daubert, Peter W. Schiller
Publikováno v: Journal of Medicinal Chemistry. 46:2104-2109
The peptide [Pro3]Dyn A(1-11)-NH2 2 exhibits high affinity (K(i) = 2.4 nM) and over 2000-fold selectivity for the opioid receptor. Stepwise removal of the C-terminal residues from this ligand demonstrated that its positively charged Arg residues, par
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::580de72a577c99e204d715451d0417e2
https://doi.org/10.1021/jm020125+
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4
Structure-activity relationships of dynorphin analogs substituted in positions 2 and 3
Autor: Jeffrey D. Daubert, Joel A. Cassel, Robert N. DeHaven, Georg Schlechtingen, Murray Goodman
Publikováno v: Biopolymers. 71:71-76
Following up on the observation that the dynorphin analog [Pro3]Dyn A(1–11)–NH2 2 possesses high affinity and selectivity for the κ opioid receptor, a number of related peptides were prepared and characterized by radioligand binding and [35S]GTP
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28be0e0bbbe6a8566d08098a0bf02048
https://doi.org/10.1002/bip.10382
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5
[Pro3]Dyn A(1−11)-NH2: A Dynorphin Analogue with High Selectivity for the κ Opioid Receptor
Autor: Jeffrey D. Daubert, Nga N. Chung, Peter W. Schiller, Li Zhang, Robert N. DeHaven, Alan Maycock, Joel A. Cassel, Murray Goodman, Georg Schlechtingen
Publikováno v: Journal of Medicinal Chemistry. 43:2698-2702
A proline scan at positions 2 and 3 of the opioid peptide dynorphin A(1-11)-NH(2) led to the discovery of the analogue [Pro(3)]Dyn A(1-11)-NH(2). This analogue possesses high affinity and selectivity for the kappa opioid receptor (K(i)(kappa) = 2.7 n
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe58c29d665db6816b13022a8d5a221a
https://doi.org/10.1021/jm990442p
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6
Evaluation of steroidal amines as lipid raft modulators and potential anti-influenza agents
Autor: Cornelia Schroeder, Hans-Joachim Knölker, Gary Jennings, Tobias Braxmeier, Sameer Agarwal, Georg Schlechtingen
Publikováno v: Bioorganicmedicinal chemistry letters. 23(18)
The influenza A virus (IFV) possesses a highly ordered cholesterol-rich lipid envelope. A specific composition and structure of this membrane raft envelope are essential for viral entry into cells and virus budding. Several steroidal amines were inve
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98514a34fc99e9a3c410a3670507e232
https://pubmed.ncbi.nlm.nih.gov/23916260
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10
Lipid-like sulfoxides and amine oxides as inhibitors of mast cell activation
Autor: Georg Schlechtingen, José Batista, Tim Friedrichson, Jürgen Bajorath, Tobias Braxmeier
Publikováno v: European journal of medicinal chemistry. 46(6)
The drug miltefosine is a prototypic lipid-like compound thought to modulate membrane environments and thereby indirectly prevent receptor-mediated signaling events. In addition to its primary therapeutic indications in cancer and leishmaniasis, milt
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64d247e9f3c4e7039008b8601eae20cf
https://pubmed.ncbi.nlm.nih.gov/21421276
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