In vitro and in vivo antifungal activities of 6-[(N-4-bromophenyl) amino]-7-chloro-5,8-quinolinediones

Abstract

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 against Aspergillus niger, Cryptococcus neoformans and Trichophyton mentagrophyte by standard agar streak method. In vitro, RCK7 showed more potent antifungal activity than fluconazole and ketoconazole. Also, RCK7 was tested for in vivo antifungal activitiy in the treatment of systemic infection with Candida 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. ED50 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 ED50 (2.05 mg/kg), the colony counts of Candida albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the ED50 (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.