Antimicrobial Agents and Chemotherapy · 2019 · 17 citations · 15 references
Life SciencesInfectious DiseasesPharmacologyAntimicrobial ResistanceDrug DiscoveryMedical MicrobiologyAntibacterial ResistanceAntibiotic ResistanceAntibiotic Resistance MechanismsMultidrug ResistanceResistance In Gram-negative BacteriaResistance In Gram-positive BacteriaFosfomycin ResistanceFosfomycin TherapyGlutathione S-transferase ActivityGlutathione S-transferase-mediated MetabolismMultidrug-resistant Gram-negative BacteriaMultidrug-resistant OrganismsMultidrug-resistant PathogensNovel Antibacterial Drug Discovery
-transferase (FosA) that metabolizes FOM. In this study, we describe the discovery and biochemical and structural characterization of ANY1 (3-bromo-6-[3-(3-bromo-2-oxo-1H-pyrazolo[1,5-a]pyrimidin-6-yl)-4-nitro-1H-pyrazol-5-yl]-1H-pyrazolo[1,5-a]pyrimidin-2-one), a small-molecule active-site inhibitor of FosA. Importantly, ANY1 potentiates FOM activity in representative Gram-negative pathogens. Collectively, our study outlines a new strategy to expand FOM activity to a broader spectrum of Gram-negative pathogens, including multidrug-resistant strains.
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Modeling of the Bacterial Growth Curve
M.H. Zwietering, I. Jongenburger, F.M. Rombouts et al. · Applied and Environmental Microbiology · 1990 · 4.2K citations · Full text
Predictive compound accumulation rules yield a broad-spectrum antibiotic
Michelle F. Richter, Bryon Drown, Andrew P. Riley et al. · Nature · 2017 · 886 citations