A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis HââRv, with MIC values ranging from 4 to 64 μg/mL. The most potent derivative 3m showed an identical MIC value of 4 μg/mL for both M. tuberculosis HââRv and rifampin-resistant M. tuberculosis 261. It demonstrated no inhibitory effects against six different tumor cell lines by a MTT assay and had a good safety profile in a vero cell line, providing a good lead for subsequent optimization in search of novel affordable antitubercular agents.
Synthesis and biological evaluation of 2-(3-fluoro-4-nitro phenoxy)-n-phenylacetamide derivatives as novel potential affordable antitubercular agents.
2-(3-氟-4-硝基苯氧基)-n-苯基乙酰胺衍生物的合成及生物学评价,作为新型潜在的廉价抗结核药物。
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| 期刊: | Molecules | 影响因子: | 4.600 |
| 时间: | 2012 | 起止号: | 2012 Feb 22; 17(2):2248-58 |
| doi: | 10.3390/molecules17022248 | ||
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