Výsledky vyhledávání - "Christian Hubschwerlen"

Discovery of Novel Inhibitors of LpxC Displaying Potent in Vitro Activity against Gram-Negative Bacteria

Publikováno v: Journal of Medicinal Chemistry. 63:66-87

UDP-3-O-((R)-3-hydroxymyristoyl)-N-glucosamine deacetylase (LpxC) is as an attractive target for the discovery and development of novel antibacterial drugs to address the critical medical need created by multidrug resistant Gram-negative bacteria. By

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eae4ad619b6cf3e0f3c6f741f71c0456
https://doi.org/10.1021/acs.jmedchem.9b01604

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Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents

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

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https://doi.org/10.1021/acs.jmedchem.6b01834

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Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria

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

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Design, Synthesis, and Characterization of Novel Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Potent Anti-Gram-Positive Activity

Autor: Daniel Bur, Azely Mirre, Michel Enderlin-Paput, Georg Rueedi, Christian Hubschwerlen, Hans H. Locher, Daniel Ritz, Cornelia Zumbrunn, Wolfgang Keck, Maria Boehme, Marina Dos Santos, Jean-Christophe Gauvin, Peter Seiler, Jean-Philippe Surivet, Verena Kaegi, Jonathan Delers, Christopher Kohl, Thierry Bruyère, Mika Gaertner

Publikováno v: Journal of Medicinal Chemistry. 56:7396-7415

There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the pote

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https://doi.org/10.1021/jm400963y

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Biomimetic Total Synthesis and Antimicrobial Evaluation of Anachelin H

Autor: Yann Bethuel, Hans Locher, Karl Gademann, Christian Hubschwerlen

Publikováno v: The Journal of Organic Chemistry. 72:8361-8370

The first biomimetic total synthesis of the iron chelator anachelin H isolated from the cyanobacterium Anabaena cylindrica is reported. A first generation approach delivered one enantiomeric series of the polyketide fragment. Comparison of the 1H NMR

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https://doi.org/10.1021/jo701402b

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Potent Algicides Based on the Cyanobacterial Alkaloid Nostocarboline

Autor: Damien Barbaras, Christian Hubschwerlen, Judith F. Blom, Karl Gademann, Hans Locher, Yann Bethuel, Tobias Brütsch

Publikováno v: Organic Letters. 8:737-740

[structure: see text] Nostocarboline and seven derivatives were prepared and displayed minimal inhibitory concentration (MIC) valuesor=100 nM against the growth of Microcystis aeruginosa PCC 7806, Synechococcus PCC 6911, and Kirchneriella contorta SA

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https://doi.org/10.1021/ol052968b

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Design, Synthesis and Biological Evaluation of Oxazolidinone–Quinolone Hybrids

Autor: Jean Luc Specklin, Christian Hubschwerlen, Hans H. Locher, Christine Sigwalt, Susanne Schroeder

Publikováno v: Bioorganic & Medicinal Chemistry. 11:2313-2319

Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesised and shown to be active against a variety of resistant and susceptible Gram-positive and fastidious Gram-negative organisms. The best

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https://doi.org/10.1016/s0968-0896(03)00083-x

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2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-Dioxo-1,4-dihydro-2H-2λ6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as Potent and Selective Peptide Deformylase Inhibitors

Autor: Michel Dietz, Frederic Marlin, Raffaello Masciadri, David Banner, Christian M. Apfel, Henri Stalder, Christian Hubschwerlen, Daniel Bur, Hans Locher, Wolfgang Pirson

Publikováno v: Journal of Medicinal Chemistry. 44:1847-1852

Potent, selective, and structurally new inhibitors of the Fe(II) enzyme Escherichia coli peptide deformylase (PDF) were obtained by rational optimization of the weakly binding screening hit (5-chloro-2-oxo-1,4-dihydro-2H-quinazolin-3-yl)-acetic acid

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https://doi.org/10.1021/jm000352g

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Peptide Deformylase as an Antibacterial Drug Target: Assays for Detection of Its Inhibition in Escherichia coli Cell Homogenates and Intact Cells

Autor: Christian Hubschwerlen, Malcolm G. P. Page, Christian M. Apfel, Wolfgang Keck, Stefan Evers, Wolfgang Pirson

Publikováno v: Antimicrobial Agents and Chemotherapy. 45:1053-1057

An assay was developed to determine the activity of peptide deformylase (PDF) inhibitors under conditions as close as possible to the physiological situation. The assay principle is the detection of N-terminal [ 35 S]methionine labeling of a protein

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https://doi.org/10.1128/aac.45.4.1053-1057.2001

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