The antifungal activities of some 6-[N-(halophenyl)amino]-7-chloro-5,8-quinolinediones against Candida species

Abstract

A series of 6-[N-(halophenyl)amino]-7-chloro-5,8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, against pathogenic Candida species such as C. albicans, C. glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halophenyl)amino]-7-chloro-5,8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5 and 7 showed more potent antifungal activities than ketoconazole. All derivatives 1-10 had specially potent activities against C. tropicalis. Derivative 1 and 2 containing (N-3,4-dihalo-phenyl)amino moiety exhibited the potent antifungal activities. Derivative 2 with (3,4-dichlorophenyl)amino substituent was the most effective in preventing the growth of Candida species at MICs 4 μg/ml respectively. © 1994 The Pharmaceutical Society of Korea.