Abstract
Lipophilic substituents at benzodioxane C (7) of 3-(benzodioxan-2-ylmethoxy)-2,6-difluorobenzamide improve the antibacterial activity against methicillin-resistant Staphylococcus aureus strains to MIC values in the range of 0.2-2.5 μg/mL, whereas hydrophilic substituents at the same position and modifications at the benzodioxane substructure, excepting for replacement with 2-cromanyl, are deleterious. Some of the lead compounds also exhibit good activity against Mtb. Parallel SARs to those of 3-(2-benzothiazol-2-ylmethoxy)-2,6-difluorobenzamide, well known FtsZ inhibitor, and cells alterations typical of FtsZ inhibition indicate such a protein as the target of these potent antibacterial benzodioxane-benzamides.
| Original language | English |
|---|---|
| Pages (from-to) | 227-243 |
| Number of pages | 17 |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 120 |
| DOIs | |
| Publication status | Published - 2016 |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- 2,6-Difluorobenzamide
- Antibacterial activity
- Benzodioxane
- FtsZ
- Methicillin resistance
- Mycobacterium tuberculosis
- Staphylococcus aureus
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