Siderophore conjugation with cleavable linkers boosts the potency of RNA polymerase inhibitors against multidrug-resistantE. coli

Author:

Peukert Carsten1ORCID,Vetter Anna C.1ORCID,Fuchs Hazel L. S.1ORCID,Harmrolfs Kirsten1ORCID,Karge Bianka1,Stadler Marc234ORCID,Brönstrup Mark135ORCID

Affiliation:

1. Department of Chemical Biology, Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124 Braunschweig, Germany

2. Department of Microbial Drugs, Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124 Braunschweig, Germany

3. German Center for Infection Research (DZIF), Site Hannover-Braunschweig, Inhoffenstraße 7, 38124 Braunschweig, Germany

4. Institute of Microbiology, Technische Universität Braunschweig, Spielmannstraße 7, 38106 Braunschweig, Germany

5. Institute for Organic Chemistry (IOC), Leibniz Universität Hannover, Schneiderberg 1B, 30167 Hannover, Germany

Abstract

RNA polymerase inhibitors against the bacteriumE. colibecome more potent when coupled to a siderophore enhancing cellular uptake, if the linker is cleaved inside the cell.

Funder

Joint Programming Initiative on Antimicrobial Resistance

Fonds der Chemischen Industrie

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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