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Synthesis and antifungal evaluation of 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones
- Synthesis and antifungal evaluation of 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones
- Ryu, CK; Choi, JA; Kim, SH
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- vol. 21, no. 4, pp. 440 - 444
- 6-(N-arylamino)-7-methylthio-5,8-quinolinedione antifungal activity; MIC minimum; inhibitory concentration; Candida species
- PHARMACEUTICAL SOCIETY KOREA
- SCIE; SCOPUS; KCI
- A series of 6-(N-arylamino)-7-methylthio-5,8-quinolined lone derivatives 4a-4l was newly synthesized for the evaluation of antifungal activity. 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones were prepared by regioselective nucleophilic substitution of 6,7-dichloro-5,8-quinolinediones with arylamines in the presence of Ce3+, and Na2S/dimethylsulfate. The MIC values of 4a-4l were determined for antifungal susceptibility in vitro against Candida species by agar streak method. The derivatives 4a-4l had generally potent antifungal activities against all human pathogenic fungi. Especially they had the most potent activity against C, krusei at 12.5 similar to 0.8 mu g/ml. Compounds 4d, 4g, 4h, 4j and 4k had more potent antifungal activities than fluconazole. Compounds 4g and 4h completely inhibited the fungal growth at 0.8 similar to 6.3 mu g/ml against all Candida species, while fluconazole inhibited the growth at 25 mu g/ml. The compounds such as 4g and 4h containing an N-(4-bromo-2-methylphenyl)- or N-(4-bromo-3-methylphenyl)amino substituent exhibited the most potent antifungal activities.
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