Patricia Schneider

TL;DR: The synthesis and characterization of 1,3-benzothiazin-4-ones (BTZs), a new class of antimycobacterial agents that kill Mycobacterium tuberculosis in vitro, ex vivo, and in mouse models of TB are described.

TL;DR: It is demonstrated that BTZs are activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1.

TL;DR: This model for testing drugs against nongrowing cells that exploits the 18b strain of M. tuberculosis 18b is proposed, a streptomycin (STR)-dependent mutant that retains significant metabolic activity in vitro, remaining positive in the resazurin reduction assay.

TL;DR: To find antimycobacterial scaffolds, a kinase inhibitor library of more than 12,000 compounds was screened using an integrated strategy involving whole cell-based assays with Corynebacterium glutamicum and Mycobacterium tuberculosis, and a target-based assay with the protein kinase PknA.

TL;DR: Nostocarboline and derivatives displayed potent and selective in vitro inhibition of P. falciparum, albeit with pronounced cytotoxicity, and three eudostomin derivatives were evaluated in an in vivo Plasmodium berghei mouse model.