Hans Gmuender

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.

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.

TL;DR: Pyrimido[1,6-alpha]benzimidazoles 11 have been found to be a new class of inhibitors of this enzyme.

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.

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.