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http://doi.org/10.25358/openscience-6261Full metadata record
| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | Barthels, Fabian | - |
| dc.contributor.author | Marincola, Gabriella | - |
| dc.contributor.author | Marciniak, Tessa | - |
| dc.contributor.author | Konhäuser, Matthias | - |
| dc.contributor.author | Hammerschmidt, Stefan | - |
| dc.contributor.author | Bierlmeier, Jan | - |
| dc.contributor.author | Distler, Ute | - |
| dc.contributor.author | Wich, Peter R. | - |
| dc.contributor.author | Tenzer, Stefan | - |
| dc.contributor.author | Schwarzer, Dirk | - |
| dc.contributor.author | Ziebuhr, Wilma | - |
| dc.contributor.author | Schirmeister, Tanja | - |
| dc.date.accessioned | 2021-08-13T07:36:00Z | - |
| dc.date.available | 2021-08-13T07:36:00Z | - |
| dc.date.issued | 2020 | - |
| dc.identifier.uri | https://openscience.ub.uni-mainz.de/handle/20.500.12030/6271 | - |
| dc.description.abstract | Staphylococcus aureus is one of the most frequent causes of nosocomial and community-acquired infections, with drug-resistant strains being responsible for tens of thousands of deaths per year. S. aureus sortase A inhibitors are designed to interfere with virulence determinants. We have identified disulfanylbenzamides as a new class of potent inhibitors against sortase A that act by covalent modification of the active-site cysteine. A broad series of derivatives were synthesized to derive structure-activity relationships (SAR). In vitro and in silico methods allowed the experimentally observed binding affinities and selectivities to be rationalized. The most active compounds were found to have single-digit micromolar Ki values and caused up to a 66 % reduction of S. aureus fibrinogen attachment at an effective inhibitor concentration of 10 μM. This new molecule class exhibited minimal cytotoxicity, low bacterial growth inhibition and impaired sortase-mediated adherence of S. aureus cells. | en_GB |
| dc.language.iso | eng | de |
| dc.rights | CC BY-NC-ND | * |
| dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
| dc.subject.ddc | 570 Biowissenschaften | de_DE |
| dc.subject.ddc | 570 Life sciences | en_GB |
| dc.title | Asymmetric disulfanylbenzamides as irreversible and selective inhibitors of Staphylococcus aureus sortase A | en_GB |
| dc.type | Zeitschriftenaufsatz | de |
| dc.identifier.doi | http://doi.org/10.25358/openscience-6261 | - |
| jgu.type.dinitype | article | en_GB |
| jgu.type.version | Published version | de |
| jgu.type.resource | Text | de |
| jgu.organisation.department | FB 09 Chemie, Pharmazie u. Geowissensch. | de |
| jgu.organisation.number | 7950 | - |
| jgu.organisation.name | Johannes Gutenberg-Universität Mainz | - |
| jgu.rights.accessrights | openAccess | - |
| jgu.journal.title | ChemMedChem | de |
| jgu.journal.volume | 15 | de |
| jgu.journal.issue | 10 | de |
| jgu.pages.start | 839 | de |
| jgu.pages.end | 850 | de |
| jgu.publisher.year | 2020 | - |
| jgu.publisher.name | Wiley-VCH | de |
| jgu.publisher.place | Weinheim u.a. | de |
| jgu.publisher.uri | https://doi.org/10.1002/cmdc.201900687 | de |
| jgu.publisher.issn | 1860-7187 | de |
| jgu.organisation.place | Mainz | - |
| jgu.subject.ddccode | 570 | de |
| jgu.publisher.doi | 10.1002/cmdc.201900687 | |
| jgu.organisation.ror | https://ror.org/023b0x485 | |
| Appears in collections: | JGU-Publikationen | |
Files in This Item:
| File | Description | Size | Format | ||
|---|---|---|---|---|---|
 | barthels_fabian-asymmetric_dis-20210805114859449.pdf | 4.18 MB | Adobe PDF | View/Open |