Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Eric A. Ertel"'
Autor:
Olivier Bezençon, Thomas Pfeifer, Johannes Mosbacher, Isabelle Reymond, Eric A. Ertel, Ruben de Kanter, Bruno Capeleto, Elvire Fournier, Markus Rey, Luca Moccia, Michael Toeroek-Schafroth, René Roscher, Richard Moon, John Gatfield, Melanie Kessler, Romain Siegrist, Bibia Heidmann, Davide Pozzi, Simon Stamm, Luboš Remeň, Sylvia Richard, Lloyd Simons, Rick Gaston, Dennis Downing, Corinna Grisostomi, Catherine Roch, Benno Schindelholz
Publikováno v:
CHIMIA, Vol 71, Iss 10 (2017)
We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemic
Externí odkaz:
https://doaj.org/article/77760779eafd425e854518b6109e1f36
Autor:
Emmanuel A. Meyer, Päivi Äänismaa, Eric A. Ertel, Eva Hühn, Daniel S. Strasser, Markus Rey, Mark J. Murphy, Marianne M. Martinic, Laetitia Pouzol, Sylvie Froidevaux, Marcel P. Keller, Eva Caroff
Publikováno v:
Journal of Medicinal Chemistry. 66:4179-4196
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a7df504f393165b1ded7be41f0a7150f
https://doi.org/10.1021/acs.jmedchem.3c00074
https://doi.org/10.1021/acs.jmedchem.3c00074
Autor:
Eric A. Ertel, Bruno Capeleto, Sylvia Richard, Olivier Bezencon, Jacques Mawet, Melanie Kessler, Thomas Pfeifer, Catherine Roch, Luboš Remeň, Richard Moon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5322-5325
We identified and characterized a series of pyrazole amides as potent, selective Ca v 3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d , with excellent potencies and/or selectivities toward the Ca v 3.2- and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::239da9b43525ccbdc87df59151643997
https://doi.org/10.1016/j.bmcl.2017.09.063
https://doi.org/10.1016/j.bmcl.2017.09.063
Autor:
Markus Gude, Georg Rueedi, Thomas Pfeifer, Christian Hubschwerlen, Daniel Ritz, Thierry Kimmerlin, L. Jacob, A.-C. Blumstein, Daniel Bur, Alain Chambovey, Lars Prade, Peter Seiler, Philippe Panchaud, Eric A. Ertel, Thierry Bruyère
Publikováno v:
Journal of Medicinal Chemistry. 60:3755-3775
Our strategy to combat resistant bacteria consisted of targeting the GyrB/ParE ATP-binding sites located on bacterial DNA gyrase and topoisomerase IV and not utilized by marketed antibiotics. Screening around the minimal ethyl urea binding motif led
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5dd48a433f27169780b7c54901c1e1ae
https://doi.org/10.1021/acs.jmedchem.6b01834
https://doi.org/10.1021/acs.jmedchem.6b01834
Autor:
Thierry Bruyère, Eric A. Ertel, Stephanie Enderlin-Paput, Hans H. Locher, Michel Enderlin-Paput, Daniel Ritz, Christopher Kohl, Jean-Christophe Gauvin, Patrick Hess, Jean-Philippe Surivet, Azely Mirre, Daniel Bur, Cornelia Zumbrunn, Georg Rueedi, Christian Hubschwerlen, Peter Seiler
Publikováno v:
Journal of Medicinal Chemistry. 60:3776-3794
There is an urgent unmet medical need for novel antibiotics that are effective against a broad range of bacterial species, especially multidrug resistant ones. Tetrahydropyran-based inhibitors of bacterial type II topoisomerases (DNA gyrase and topoi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03730300d43232dbf6451dab25886d78
https://doi.org/10.1021/acs.jmedchem.6b01831
https://doi.org/10.1021/acs.jmedchem.6b01831
Autor:
Romain Sube, Eric A. Ertel
Publikováno v:
Journal of Biomedical Science and Engineering. 10:527-549
Introduction: Cardiomyocytes derived from human induced pluripotent stem cells (hiPSC-CM) form spontaneously beating syncytia in-vitro. We evaluated whether hiPSC-CM are a compelling model of human cardiac pharmacology useful for early drug developme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e05b711ee41ca118a9a522c7c3b92361
https://doi.org/10.4236/jbise.2017.1011040
https://doi.org/10.4236/jbise.2017.1011040
Autor:
Melanie Kessler, Eric A. Ertel, John Gatfield, Rick D Gaston, Corinna Grisostomi, Thomas Pfeifer, Lubos Remen, Lloyd Simons, Olivier Bezencon, Johannes Mosbacher, Catherine Roch, Richard Moon, Dennis Michael Downing, Markus Rey
Publikováno v:
Journal of Medicinal Chemistry. 59:8398-8411
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij ra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f1d15b224e97575ffd39760a63e490e
https://doi.org/10.1021/acs.jmedchem.6b00756
https://doi.org/10.1021/acs.jmedchem.6b00756
Publikováno v:
Journal of Visualized Experiments : JoVE
Spontaneously contracting syncytia of cardiomyocytes derived from human-induced pluripotent stem cells (hiPSC-CM) are a useful model of human cardiac physiology and pharmacology. Various methods have been proposed to record this spontaneous activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cfbb80eb078d56ef4ce24bf4a2d9473
https://doi.org/10.3791/58290
https://doi.org/10.3791/58290
Autor:
Olivier, Bezençon, Luboš, Remeň, Sylvia, Richard, Catherine, Roch, Melanie, Kessler, Eric A, Ertel, Richard, Moon, Jacques, Mawet, Thomas, Pfeifer, Bruno, Capeleto
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(23)
We identified and characterized a series of pyrazole amides as potent, selective Ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::d9b2a0a0237f0f2b76d7bcd37b74d58f
https://pubmed.ncbi.nlm.nih.gov/29066309
https://pubmed.ncbi.nlm.nih.gov/29066309
Autor:
Frances M. Platt, Marc Iglarz, Eric A. Ertel, Daniela Baldoni, Richard W. D. Welford, Caroline Deymier, Markus R. Probst, David A. Priestman, Andreas Mühlemann, Marco Garzotti
Publikováno v:
Molecular Genetics and Metabolism. 120:S139-S140
Fabry disease (FD) is a lysosomal disorder caused by mutations in the GLA gene coding for α‑galactosidase A (α‑GalA). These mutations lead to the accumulation of α‑GalA substrates, including globotriaosylceramide (Gb3). As a consequence of l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ce03a0f6c08adc66569b7dcaee14962
https://doi.org/10.1016/j.ymgme.2016.11.369
https://doi.org/10.1016/j.ymgme.2016.11.369