Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI

Uropathogenic E. coli (UPEC) employ the mannose-binding adhesin FimH to colonize the bladder epithelium during urinary tract infection (UTI). Previously reported FimH antagonists exhibit good potency and efficacy, but low bioavailability and a short half-life in vivo. In a rational design strategy,...

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Veröffentlicht in:ChemMedChem
Hauptverfasser: Jarvis, Cassie, Han, Zhenfu, Kalas, Vasilios, Klein, Roger, Pinkner, Jerome S., Ford, Bradley, Binkley, Jana, Cusumano, Corinne K., Cusumano, Zachary, Mydock-McGrane, Laurel, Hultgren, Scott J., Janetka, James W.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2016
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4818977/
https://ncbi.nlm.nih.gov/pubmed/26812660
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cmdc.201600006
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