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

• 영문명: The Evaluation of Antifungal Activities and Safeties of 6-[(N-3,4-Difluorophenyl)amino]-7-Chloro-5,8-Quinolinedione
• 발행기관: 대한약학회
• 저자명: 유충규(Chung Kyu Ryu) 김동현(Dong Hyun Kim) 윤여표(Yeo Pyo Yun) 이병무(Byung Mu Lee) 허문영(Moon Young Heo) 정해문(Hae Moon Chung) 권상미(Sang Mee Kwon) 정성희(Sung Hee Jung)
• 간행물 정보: 『약학회지』제40권 제5호 (1996년), 608~615쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1996.10.31

영문 초록

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 ED50, 0.30 +/- 0.14mg/kg but ketoconazole and fluconazole had ED50, 8.00 +/- 0.73, 10.00 +/- 0.43mg/kg respectively. Intraperitoneally administered RCK3 at the ED50 for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver as well as ketoconazole and fluconazole at these ED50. And administered RCK4 at the ED50 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 LD50 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.

키워드

6-[(N-4-Difluorophenyl)-amino]-7-chloro-5.8-quinolinedione in vivo Candida albicans antifungal acute toxicity chromosomal aberration test Ames test micronncleus assay.