H
Hans Gmuender
Researcher at Hoffmann-La Roche
Publications - 11
Citations - 803
Hans Gmuender is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: DNA gyrase & Antibacterial agent. The author has an hindex of 7, co-authored 11 publications receiving 779 citations.
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Journal ArticleDOI
Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening.
Hans-Joachim Boehm,Markus Boehringer,Daniel Bur,Hans Gmuender,Walter Huber,Werner Klaus,Dirk Kostrewa,Holger Kuehne,Thomas Luebbers,Nathalie Meunier-Keller,Francis Mueller +10 more
TL;DR: This work combines as key techniques an in silico screening for potential low molecular weight inhibitors, a biased high throughput DNA gyrase screen, validation of the screening hits by biophysical methods, and a 3D guided optimization process.
Journal ArticleDOI
Gene Expression Changes Triggered by Exposure of Haemophilus influenzae to Novobiocin or Ciprofloxacin: Combined Transcription and Translation Analysis
TL;DR: Treatment with the ATPase inhibitor Novobiocin changed the expression rates of many genes, reflecting the fact that the initiation of transcription for many genes is sensitive to DNA supercoiling.
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Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors.
Christian Hubschwerlen,Philippe Pflieger,Jean-Luc Specklin,Klaus Gubernator,Hans Gmuender,Peter Angehrn,Ivan Kompis +6 more
TL;DR: Pyrimido[1,6-alpha]benzimidazoles 11 have been found to be a new class of inhibitors of this enzyme.
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New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine
Peter Angehrn,Stefan Buchmann,Christoph Funk,Erwin Goetschi,Hans Gmuender,Paul Hebeisen,Dirk Kostrewa,Helmut Link,Thomas Luebbers,Raffaello Masciadri,Joergen Nielsen,Peter Reindl,Fabienne Ricklin,§ and Anne Schmitt-Hoffmann,Frank-Peter Theil +14 more
TL;DR: Improving the pharmacokinetic properties of the most active compounds, in particular by lowering their lipophilic properties, was able to identify congeners of cyclothialidine that showed efficacy in vivo, and a modification program afforded a number of inhibitors that showed in vitro activity against Gram-positive bacteria.
Journal ArticleDOI
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
Peter Angehrn,Erwin Goetschi,Hans Gmuender,Paul Hebeisen,Michael Hennig,Bernd Kuhn,Thomas Luebbers,Peter Reindl,Fabienne Ricklin,Anne Schmitt-Hoffmann +9 more
TL;DR: After adjusting their lipophilicity by methyl-halogen exchange at the benzene ring, compounds of this series did not require the thioamide functionality to exert a decent antibacterial potency and consequently exhibited improved pharmacokinetic properties resulting in a pronounced in vivo efficacy in a mouse septicaemia infection model.