In vitro andin vivo antifungal activities of 6-[(N-4-bromophenyl) amino]-7-chloro-5,8-quinolinediones.
Antifungal activities of 6-[(N-4-bromophenyl)amino]-7-chloro-5,8-quinolinedione (RCK7) were tested. The MIC values of RCK7 were determined for antifungal suceptibility,in vitro againstAspergillus niger, Cryptococcus neoformans andTrichophyton mentagrophyte by standard agar streak method.In vitro, RCK7 showed more potent antifungal activity than fluconazole and ketoconazole. Also, RCK7 was tested forin vivo antifungal activity in the treatment of systemic infection withCandida albicans in normal mice. The therapeutic potential of RCK7 had been assessed by evaluating their survival rate against systemic infections compared with that of ketoconazole. ED(50) of intraperitoneally administered RCK7 was 2.05+/-0.30 mg/kg but that of ketoconazole was 8.00+/-0.73 mg/kg, respectively. When RCK7 was administered intravenously at the ED(50) (2.05 mg/kg), the colony counts ofCandida albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the ED(50) (8.00 mg/kg), and the better survival rates than ketoconazole's were achieved after 14 days. The results suggest that RCK7 may be a potent antifungal agent.
Ryu
C K
CK
College of Pharmacy, Ewha Womans University, Sodaemun-Ku, 120-750, Seoul, Korea.
Kim
D H
DH
Kwon
S M
SM
Jung
S H
SH
Kim
S H
SH