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dc.contributor.authorDreger, Alexander
dc.contributor.authorHoff, Katharina
dc.contributor.authorAgoglitta, Oriana
dc.contributor.authorHotop, Sven-Kevin
dc.contributor.authorBrönstrup, Mark
dc.contributor.authorHeisig, Peter
dc.contributor.authorKirchmair, Johannes
dc.contributor.authorHoll, Ralph
dc.date.accessioned2021-01-26T11:44:02Z
dc.date.available2021-01-26T11:44:02Z
dc.date.issued2020-12-31
dc.identifier.citationBioorg Chem. 2020 Dec 31;107:104603. doi: 10.1016/j.bioorg.2020.104603. Epub ahead of print.en_US
dc.identifier.pmid33429229
dc.identifier.doi10.1016/j.bioorg.2020.104603
dc.identifier.urihttp://hdl.handle.net/10033/622699
dc.description.abstractLpxC inhibitors represent a promising class of novel antibiotics selectively combating Gram-negative bacteria. In chiral pool syntheses starting from D- and L-xylose, a series of four 2r,3c,4t-configured C-furanosidic LpxC inhibitors was obtained. The synthesized hydroxamic acids were tested for antibacterial and LpxC inhibitory activity, the acquired biological data were compared with those of previously synthesized C-furanosides, and molecular docking studies were performed to rationalize the observed structure-activity relationships. Additionally, bacterial uptake and susceptibility to efflux pump systems were investigated for the most promising stereoisomers.en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectAntibioticsen_US
dc.subjectBacterial uptakeen_US
dc.subjectC-glycosidesen_US
dc.subjectLpxC inhibitorsen_US
dc.subjectMolecular docking studiesen_US
dc.titleAntibacterial activity of xylose-derived LpxC inhibitors - Synthesis, biological evaluation and molecular docking studies.en_US
dc.typeArticleen_US
dc.identifier.eissn1090-2120
dc.contributor.departmentHZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany.en_US
dc.identifier.journalBioorganic chemistryen_US
dc.source.volume107
dc.source.beginpage104603
dc.source.endpage
dc.source.journaltitleBioorganic chemistry
dc.source.countryUnited States


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