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

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 ant...

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Veröffentlicht in:	Archives of pharmacal research 2002-12, Vol.25 (6), p.795-800
Hauptverfasser:	Ryu, Chung -Kyu, Sun, Yang -Jung, Shim, Ju -Yeon, You, Hea -Jung, Choi, Ko Un, Lee, Heesoon
Format:	Artikel
Sprache:	eng
Schlagworte:	Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology antifungal properties Aspergillus niger - drug effects Candida albicans - drug effects flucytosine fungi Microbial Sensitivity Tests - statistics & numerical data Quinolines - chemical synthesis Quinolines - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0253-6269 1976-3786
DOI:	10.1007/BF02976994