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Synthesis and antifungal activity of 6,7-bis-[s-(aryl)thio]-5,8-quinolinediones

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Abstract

6,7-Bis-[S-(aryl)thio]-5,8-quinolinediones4 and5 were synthesized by the substitution of 6,7-dichloro-5,8-quinolinediones with appropriate arylthiols. Their antifungal activity were testedin vitro for their growth inhibitory activities against pathogenic fungi in comparison with flucytosine. The antifungal activities were significantly improved by S-(aryl)thio moieties of the compounds4 and5. The all tested compounds4 and5 showed generally good activities againstC. albicans andA. niger ranging from 0.8 to 25 μg/ml. Among them, compounds4d-4h and5a-5c exhibited also good activities againstC. krusei andC. tropicalis. The activities of compounds4j and41 were comparable to those of flucytosine against all tested fungi.

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Correspondence to Chung -Kyu Ryu.

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Ryu, C.K., Sun, Y.J., Shim, J.Y. et al. Synthesis and antifungal activity of 6,7-bis-[s-(aryl)thio]-5,8-quinolinediones. Arch Pharm Res 25, 795–800 (2002). https://doi.org/10.1007/BF02976994

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