Synthesis and antifungal activity of 6,7-bis-[S-(aryl)thio]-5,8-quinolinediones.
6,7-Bis-[S-(aryl)thio]-5,8-quinolinediones 4 and 5 were synthesized by the substitution of 6,7-dichloro-5,8-quinolinediones with appropriate arylthiols. Their antifungal activity were tested in 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 compounds 4 and 5. The all tested compounds 4 and 5 showed generally good activities against C. albicans and A. niger ranging from 0.8 to 25 microg/ml. Among them, compounds 4d-4h and 5a-5c exhibited also good activities against C. krusei and C. tropicalis. The activities of compounds 4j and 4l were comparable to those of flucytosine against all tested fungi.
Ryu
Chung-Kyu
CK
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120-750, Korea. ckryu@mm.ewha.ac.kr
Sun
Yang-Jung
YJ
Shim
Ju-Yeon
JY
You
Hea-Jung
HJ
Choi
Ko Un
KU
Lee
Heesoon
H
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001234:Aspergillus niger / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D011804:Quinolines