6- [(Halopheny1) amino]-7-Bromo-5,8-Quinolinediones Treatment of Candidiasis in Normal Mice

  • Published : 1996.04.01

Abstract

A series of 6-[(N-Halophenyl)amino] -7-Bromo-5,8-quinolinediones (BQs) newly synthesized were tested for antifungal activities, in vitro, against Candida sp., Aspergillus niger and Trichophyton mentagrophytes. The MIC values were determined by the twofold dilution method. Among these derivatives, BQ4 and 7 showed more potent antifungal activities than fluconazole and ketoconazole. BQ 4 and 7 were compared with fluconazole in the treatment of established systemic infections with Candida albicans in normal rats. Intraperitoneally administered BQs for 7 days and 14 days reduced Candida albicans colony count in kidneys and livers as well as fluconazole. The therapeutic potential of BQs has been assessed by evaluating their activities (survival rate) against systemic infections in normal mice with Candida albicans. These compounds, particularly showed activities comparable with fluconazole. BQ4 and 7 had about EO$\_$50/, 0.05, 0.06mg/kg but fluconazole had ED$\_$50/, 6.0mg/kg respectively.

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