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New fluorine-containing hydrazones active against MDR-tuberculosis
Eva Vavříková, Slovenko Polanc, Marijan Kočevar, Kata Horváti, Szilvia Bősze, Jiřina Stolaříková, Kateřina Vávrová, Jarmila Vinšová
Jazyk angličtina Země Francie
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
NS10367
MZ0
CEP - Centrální evidence projektů
- 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
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.
Institute of Public Health Centre of Hygienic Laboratories Ostrava Czech Republic
University of Ljubljana Faculty of Chemistry and Chemical Technology Ljubljana Slovenia
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- $a 10.1016/j.ejmech.2011.07.052 $2 doi
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- $a 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.
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- $a Polanc, Slovenko $u University of Ljubljana, Faculty of Chemistry and Chemical Technology, Ljubljana, Slovenia
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- $a Kočevar, Marijan $u University of Ljubljana, Faculty of Chemistry and Chemical Technology, Ljubljana, Slovenia
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- $a Horváti, Kata $u Eötvös Loránd University, Research Group of Peptide Chemistry, Hungarian Academy of Science, Budapest, Hungary
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- $a Bosze, Szilvia $u Eötvös Loránd University, Research Group of Peptide Chemistry, Hungarian Academy of Science, Budapest, Hungary
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- $w MED00001628 $t European journal of medicinal chemistry $x 1768-3254 $g Roč. 46, č. 10 (2011), s. 4937-4945
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