Antibacterial activity of xylose-derived LpxC inhibitors - Synthesis, biological evaluation and molecular docking studies.
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Authors
Dreger, AlexanderHoff, Katharina
Agoglitta, Oriana
Hotop, Sven-Kevin
Brönstrup, Mark

Heisig, Peter
Kirchmair, Johannes
Holl, Ralph
Issue Date
2020-12-31
Metadata
Show full item recordAbstract
LpxC 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.Citation
Bioorg Chem. 2020 Dec 31;107:104603. doi: 10.1016/j.bioorg.2020.104603. Epub ahead of print.Affiliation
HZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany.Publisher
ElsevierJournal
Bioorganic chemistryPubMed ID
33429229Type
ArticleLanguage
enEISSN
1090-2120ae974a485f413a2113503eed53cd6c53
10.1016/j.bioorg.2020.104603
Scopus Count
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- Creative Commons
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 International
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