• Archives of Pharmacal Research
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• 제17권6호
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• pp.483-486
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• 1994

A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, 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-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)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 kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

• Biomolecules & Therapeutics
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• 제3권3호
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• pp.182-187
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• 1995

The clastogenecity and mutagenicity of antifungal 6-[(N-halophenyl)amino]-7-chloro-5, 8-quinolinedione (RCK 3, 7, 13, 14, and 15) had been evaluated. Salmonella typhimurium reversion assay (Ames test) was used to test the mutagenicity of RCKs. RCK14 was mutagenic in S. typhimurium(TA98 and TA100) with and without rat liver microsomal activation. Whereas RCK3, 7, 13 and 15 were negative in Ames test with Salmonella typhimurium(TA98 and TA100), The clastogenecity was tested on the RCKs with in vivo mouse micronucleus assay. All of RCKs tested did not show any clastogenic effect in mouse peripheral blood. Thus RCKs were not supposed to cause any chromosomal damage termed micronuclei. These results indicate that RCK 3, 7, 13 and 15 have no genotoxic potential under these experimental condition.