Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Dirk Behnke"'
Autor:
Claudia Betschart, Michael Faller, Florence Zink, René Hemmig, Jutta Blank, Eric Vangrevelinghe, Marjorie Bourrel, Ralf Glatthar, Dirk Behnke, Kerstin Barker, Andreas Heizmann, Daniela Angst, Pierre Nimsgern, Sébastien Jacquier, Tobias Junt, Géraldine Zipfel, Giulia Ruzzante, Pius Loetscher, Sarah Limonta, Stuart Hawtin, Cedric Bernard Andre, Thomas Boulay, Roland Feifel, Thomas Knoepfel
Publikováno v:
ACS Med Chem Lett
[Image: see text] Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. Here we report on the efficient structure-based optimization of the inhibition of TLR8, starting from a co-crystal stru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33fee8bacdcd6ab213f658c3a1348d56
https://doi.org/10.1021/acsmedchemlett.1c00696
https://doi.org/10.1021/acsmedchemlett.1c00696
Autor:
Jonathan A. Deane, Stuart Hawtin, Roland Feifel, Pius Loetscher, Sarah Limonta, Tobias Junt, Ralf Glatthar, Michellys Pierre-Yves, Marjorie Bourrel, Thomas Knoepfel, Cedric Bernard Andre, Thomas Boulay, Pierre Nimsgern, Sebastien Jacquier, Eric Vangrevelinghe, Michael Faller, Claudia Betschart, Jutta Blank, Phillip B. Alper, Geraldine Collignon Zipfel, Dirk Behnke
Publikováno v:
Journal of Medicinal Chemistry. 63:8276-8295
Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition assay and its application for hit generation of dual
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98a6d30a18c77cefd130b9738cd75108
https://doi.org/10.1021/acs.jmedchem.0c00130
https://doi.org/10.1021/acs.jmedchem.0c00130
Autor:
Arndt Meyer, Murali Chebrolu, Christine E. Gee, Grit Laue, Markus Fendt, Laura H. Jacobson, Sangamesh Badiger, Samuel Hintermann, Chetan Pandit, Simona Cotesta, Claudia Betschart, Daniel Hoyer, Vinod D. Chaudhari, Dirk Behnke, Trixie Wagner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5555-5560
Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::683f840d5741ac67440ee89e98efc728
https://doi.org/10.1016/j.bmcl.2015.10.055
https://doi.org/10.1016/j.bmcl.2015.10.055
Autor:
Chetan Pandit, Christine E. Gee, Daniel Hoyer, Vinod D. Chaudhari, Grit Laue, Juergen Wagner, Laura H. Jacobson, Dirk Behnke, Claudia Betschart, Simona Cotesta, Sangamesh Badiger, Samuel Hintermann, Markus Fendt, Silvio Ofner
Publikováno v:
Journal of Medicinal Chemistry. 56:7590-7607
Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clinical trials in volunteers and primary insomnia patients. The r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48dc21e46c9f923dccf5394833956e52
https://doi.org/10.1021/jm4007627
https://doi.org/10.1021/jm4007627
Autor:
Ivo Vranesic, Peter Ertl, Manuel Koller, Grit Laue, Dirk Behnke, David Orain, Sandrine Desrayaud, David Carcache
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6454-6459
1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic scaffold allowed to improve the physico-chemical parameters for optimization of the aqueous
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fc51fe950ab99a627e4927771bfbf5e
https://doi.org/10.1016/j.bmcl.2012.08.053
https://doi.org/10.1016/j.bmcl.2012.08.053
Publikováno v:
Synlett. :688-692
A novel three-component, one-pot reaction between primary (S)-amino acid amides, aldehydes and isocyanides in the presence of acetic acid yielding substituted 2-(cyanomethylamino)-acetamides 4 in good yields, is described. First efforts to investigat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::289bb6257bb7d09d655eb3fe108dae73
https://doi.org/10.1055/s-2004-817764
https://doi.org/10.1055/s-2004-817764
Autor:
Silvio Ofner, Dirk Behnke, Edi Schuepbach, Christine E. Gee, Morenike Olorunda, Samuel Hintermann, Markus Fendt, Emmanuelle Briard, Daniel Langenegger, Daniel Hoyer, Grit Laue, Gabrielle E. Callander, Laura H. Jacobson, Claudia Betschart, Simona Cotesta, Dominique Monna
Publikováno v:
Frontiers in Neuroscience
Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in clinical settings and thorough investigations of pharmacokinetics and pharmacodynamics can pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56c48587021d06fac0335b5334a7b2ec
Autor:
Dirk Behnke, Lothar Hennig, Matthias Findeisen, Peter Welzel, Dietrich Müller, Michael Thormann, Hans-Jörg Hofmann
Publikováno v:
Tetrahedron. 56:1081-1095
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::56e233d4b9fba28f6945b8883dc913ac
https://doi.org/10.1016/s0040-4020(00)00005-3
https://doi.org/10.1016/s0040-4020(00)00005-3
Publikováno v:
Tetrahedron Letters. 38:7059-7062
InCl 3 -mediated coupling of δ-alkoxy allylic stannane 9b with aldehydes has been shown to give the α-coupling products in high yield, probably via two S e ′ processes. Most specifically, drimenal ( rac- 1 ) has been converted into labdane deriva
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1b7f93ffc848d4ce6f70977310a4438c
https://doi.org/10.1016/s0040-4039(97)01662-6
https://doi.org/10.1016/s0040-4039(97)01662-6
Publikováno v:
ChemInform. 29
InCl 3 -mediated coupling of δ-alkoxy allylic stannane 9b with aldehydes has been shown to give the α-coupling products in high yield, probably via two S e ′ processes. Most specifically, drimenal ( rac- 1 ) has been converted into labdane deriva
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::451d8b31b6594ebf11dc5a153650de0a
https://doi.org/10.1002/chin.199802053
https://doi.org/10.1002/chin.199802053