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Structural Variations in the Central Heterocyclic Scaffold of Tripartite 2,6-Difluorobenzamides: Influence on Their Antibacterial Activity against MDR <i>Staphylococcus aureus</i>
oleh: Thibaut Barbier, Cédric Badiou, Floriane Davy, Yves Queneau, Oana Dumitrescu, Gérard Lina, Laurent Soulère
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2022-10-01 |
Deskripsi
Five series of heterocyclic tripartite 2,6-difluorobenzamides, namely 1,2,3-triazoles, 1,2,4- and 1,3,4-oxadiazoles, analogs of reported model anti-staphylococcal compounds, were prepared. The purpose was to investigate the influence of the nature of the heterocyclic central scaffold on the biological activity against three strains of <i>S. aureus,</i> including two drug-resistant ones. Among the 15 compounds of the new collection, a 3-(4-<i>tert</i>-butylphenyl)-1,2,4-oxadiazole linked via a methylene group with a 2,6-difluorobenzamide moiety (<b>II.c</b>) exhibited a minimal inhibitory concentration between 0.5 and 1 µg/mL according to the strain. Subsequent studies on <b>II.c</b> demonstrated no human cytotoxicity, while targeting the bacterial divisome.