Journal
MOLECULES
Volume 27, Issue 19, Pages -Publisher
MDPI
DOI: 10.3390/molecules27196619
Keywords
azoles; antibacterial; Staphylococcus aureus; benzamide
Funding
- CNRS
- MESRI
- INSERM
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In this study, five series of heterocyclic tripartite 2,6-difluorobenzamides were synthesized to investigate the influence of the nature of the heterocyclic central scaffold on the biological activity against Staphylococcus aureus. Among the compounds, II.c showed low minimum inhibitory concentration and exhibited no cytotoxicity against human cells.
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 S. aureus, including two drug-resistant ones. Among the 15 compounds of the new collection, a 3-(4-tert-butylphenyl)-1,2,4-oxadiazole linked via a methylene group with a 2,6-difluorobenzamide moiety (II.c) exhibited a minimal inhibitory concentration between 0.5 and 1 mu g/mL according to the strain. Subsequent studies on II.c demonstrated no human cytotoxicity, while targeting the bacterial divisome.
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