Synthesis and in vitro antimycobacterial activity of 2-methoxybenzanilides and their thioxo analogues
Language English Country France Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
22907036
DOI
10.1016/j.ejmech.2012.07.044
PII: S0223-5234(12)00470-9
Knihovny.cz E-resources
- MeSH
- Anilides chemical synthesis chemistry pharmacology MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Hep G2 Cells MeSH
- Enzyme Inhibitors chemical synthesis chemistry pharmacology MeSH
- Isocitrate Lyase antagonists & inhibitors metabolism MeSH
- Humans MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium avium drug effects MeSH
- Mycobacterium kansasii drug effects MeSH
- Mycobacterium tuberculosis drug effects MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Drug Screening Assays, Antitumor MeSH
- Cell Survival drug effects MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anilides MeSH
- Anti-Bacterial Agents MeSH
- Enzyme Inhibitors MeSH
- Isocitrate Lyase MeSH
- Antineoplastic Agents MeSH
A new series of N-(3/4-substituted phenyl) 4/5-chloro-2-methoxybenzamides and their thioxo analogues have been synthesised and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv, as well as the two atypical strains Mycobacterium kansasii and Mycobacterium avium. Five of the most active compounds were evaluated for cytotoxicity and their ability to inhibit mycobacterial isocitrate lyase, which is responsible for latent survival of Mycobacterium. The results showed that benzthioanilides were more active than the corresponding benzanilides. The most active compound, 4-chloro-2-methoxy-N-(3,4-dichlorophenyl)benzothioamide (4e), had a minimal inhibition concentration (MIC) against M. tuberculosis of 2 μmol L(-1), which was better than the activity of the previously published corresponding salicylanilide.
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