• Archives of Pharmacal Research
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• v.17 no.6
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• pp.483-486
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• 1994

A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, C glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)amino]-7-chloro-5, 8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5, and 7 showed more potent antifungal activities than kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

• YAKHAK HOEJI
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• v.42 no.5
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• pp.527-533
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• 1998

6-(3,4-Dichlorophenyl)amino-7-chloro-5,8-quinolinedione (RCK50) was tested for antifungal activities in mice systemically infected with Candida albicans. The therapeutic potential of RCK50 was also assessed in comparison with ketoconazole. CK50 had $ED_{50}$ 0.22${\pm}$0.01mg/kg. Ketoconazole as a positive control had $ED_{50}$ 6.00${\pm}$1.70mg/kg. Intraperitoneally administered RCK50 at the $ED_{50}$ for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver. And administered RCK50 at the $ED_{50}$ for 14 days improved survival rates. The genotoxicities of RCK50 had been evaluated. RCK50 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. RCK50 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK50 has no genotoxic potential under these experimental conditions. Acute oral toxicity studies of RCK50 were carried out in ICR mice of both sexes. RCK50 did not show acute oral toxicities and $LD_{50}$ values were over 2,850mg/kg in ICR mice.