Vincent Gerusz

TL;DR: The approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2- Daryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-ones identified by virtual screening are reported.

TL;DR: In vivo, MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/ kg/day), and support MUT56399 as a very promising candidate for a novel drug to treat severe staphylococcal infections.

TL;DR: Development of a biochemical assay suitable for high-throughput screening allowed the discovery of inhibitors 1 and 2 of HldE kinase, which led to highly potent compounds.

TL;DR: This study describes the first inhibitors of GmhA ever reported, and paves the way to the design of a second generation of molecules targeting the bacterial virulence.

TL;DR: Some elements of the optimization program to decouple triclosan's specific FabI effect from its nonspecific cytotoxic component delivered highly specific, potent, and nonbiocidal new FabI inhibitors.