The Evaluation of Antifungal Activities and Safeties of 6-[(N-3,4-Difluorophenyl)amino]-7-Chloro-5,8-Quinolinedione

6-[(N-3,4-디플루오로페닐)아미노]-7-클로로-5,8-퀴놀린디온의 항진균작용 및 안전성 평가

6-[(N-3,4-Difluorophenyl)amino]-7-chloro-5,8-quinolinedione(RCK4) was tested for antifungal activities, against systemic infections with Candida albicans in normal mice. The therapeutic potential of RCK4 had been assessed in comparison with ketoconazole and fluconazole. RCK4 had $ED_{50},\;0.30{\pm}0.14$ but ketoconazole and fluconazole had $ED_{50},\;8.00{\pm}0.73,\;10.00{\pm} 0.43mg/kg$ respectively. Intraperitoneally administered RCK3 at the $ED_{50}$ for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver as well as ketoconazole and fluconazole at these $ED_{50}$. And administered RCK4 at the $ED_{50}$ for 14 days improved survival rates as well as ketoconazole. Acute oral toxicity studies of RCK4 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK4 were low and $LD_{50}$ values were over 2,850mg/kg in ICR mice. The genotoxicities of RCK4 had been evaluated. RCK4 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK4 with in vivo mouse micronucleus assay. RCK4 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK4 has no genotoxic potential under these experimental conditions.