|
KMID : 0043319980210040440
|
|
Archives of Pharmacal Research
1998 Volume.21 No. 4 p.440 ~ p.444
|
|
|
Synthesis and Antifungal Evaluation of 6-(N-arylamino)-7-methylthio-5,8-quinolinediones
|
|
Kim Chung-Kyu
Choi Jung-Ah
Kim Sung-Hee
|
|
|
Abstract
|
|
|
|
A series of 6-(N-arylamino)-7-methylthio-5,8-quinolinedione 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 , and S/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 12.5-0.8 /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 0.8-6.3 /ml against all Candida species, while fluconazole inhibited the growth at 25 /ml. The compounds such as 4g and 4h containing an N-(4-bromo-2-methylphenyl)- or N-(4-bromo-3methylphenyl)amino substituent exhibited the most potent antifungal activities.
|
|
|
KEYWORD
|
|
|
6-(N-Arylamino)-7-methylthio-5, 8-quinolinedione, Antifungal activity, MIC minimum inhibitory concentration, Candida species
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|
|