New fluorine-containing hydrazones active against MDR-tuberculosis
Jazyk angličtina Země Francie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
21855181
DOI
10.1016/j.ejmech.2011.07.052
PII: S0223-5234(11)00565-4
Knihovny.cz E-zdroje
- MeSH
- antituberkulotika chemie metabolismus farmakologie MeSH
- buněčné linie MeSH
- fluor chemie metabolismus farmakologie MeSH
- hydrazony chemie metabolismus farmakologie MeSH
- krevní plazma metabolismus MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- multirezistentní tuberkulóza farmakoterapie MeSH
- Mycobacterium kansasii účinky léků MeSH
- Mycobacterium účinky léků MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- antituberkulotika MeSH
- fluor MeSH
- hydrazony MeSH
Several new fluorine-containing hydrazones were synthesized and screened for their in vitro antimycobacterial activity. Nine of these derivatives have shown a remarkable activity against MDR-TB strain with MIC 0.5 μg/mL and high value of selectivity index (SI). Compound 3h with the highest SI (1268.58) was used for stability evaluation with putative metabolites (ciprofloxacin and formylciprofloxacin) detection. Compound 3h was stable at pH 7.4 of aqueous buffer and rat plasma, in acidic buffers (at pH 3 and 5) slow decomposition was observed. Interestingly, no formylciprofloxacin was detected in the solution, and only slightly increased concentration of ciprofloxacin was observed instead. Trifluoromethyl hydrazones 3f and 3g exhibited the best activity also against two strains of Mycobacterium kansasii (MIC 1-4 μmol/L). All evaluated compounds were found to be non-cytotoxic.
Citace poskytuje Crossref.org
N-substituted 2-isonicotinoylhydrazinecarboxamides--new antimycobacterial active molecules