Antibacterial activity of xylose-derived LpxC inhibitors - Synthesis, biological evaluation and molecular docking studies.
dc.contributor.author | Dreger, Alexander | |
dc.contributor.author | Hoff, Katharina | |
dc.contributor.author | Agoglitta, Oriana | |
dc.contributor.author | Hotop, Sven-Kevin | |
dc.contributor.author | Brönstrup, Mark | |
dc.contributor.author | Heisig, Peter | |
dc.contributor.author | Kirchmair, Johannes | |
dc.contributor.author | Holl, Ralph | |
dc.date.accessioned | 2021-01-26T11:44:02Z | |
dc.date.available | 2021-01-26T11:44:02Z | |
dc.date.issued | 2020-12-31 | |
dc.identifier.citation | Bioorg Chem. 2020 Dec 31;107:104603. doi: 10.1016/j.bioorg.2020.104603. Epub ahead of print. | en_US |
dc.identifier.pmid | 33429229 | |
dc.identifier.doi | 10.1016/j.bioorg.2020.104603 | |
dc.identifier.uri | http://hdl.handle.net/10033/622699 | |
dc.description.abstract | 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. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 International | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Antibiotics | en_US |
dc.subject | Bacterial uptake | en_US |
dc.subject | C-glycosides | en_US |
dc.subject | LpxC inhibitors | en_US |
dc.subject | Molecular docking studies | en_US |
dc.title | Antibacterial activity of xylose-derived LpxC inhibitors - Synthesis, biological evaluation and molecular docking studies. | en_US |
dc.type | Article | en_US |
dc.identifier.eissn | 1090-2120 | |
dc.contributor.department | HZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany. | en_US |
dc.identifier.journal | Bioorganic chemistry | en_US |
dc.source.volume | 107 | |
dc.source.beginpage | 104603 | |
dc.source.endpage | ||
dc.source.journaltitle | Bioorganic chemistry | |
dc.source.country | United States |