View : 16 Download: 0

Synthesis and antifungal evaluation of 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones

Title
Synthesis and antifungal evaluation of 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones
Authors
Ryu, CKChoi, JAKim, SH
Ewha Authors
유충규
SCOPUS Author ID
유충규scopus
Issue Date
1998
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
ISSN
0253-6269JCR Link
Citation
vol. 21, no. 4, pp. 440 - 444
Keywords
6-(N-arylamino)-7-methylthio-5,8-quinolinedione antifungal activityMIC minimuminhibitory concentrationCandida species
Publisher
PHARMACEUTICAL SOCIETY KOREA
Indexed
SCIE; SCOPUS; KCI WOS scopus
Abstract
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.
DOI
10.1007/BF02974640
Appears in Collections:
약학대학 > 약학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE