Synthesis and antifungal activity of 6-arylthio-/6-arylamino-4,7-dioxobenzothiazoles.
6-Arylthio-/6-arylamino-4,7-dioxobenzothiazoles were synthesized and tested for in vitro antifungal activity against Candida species and Aspergillus niger. 6-Arylamino-4,7-dioxobenzothiazoles 5 and 6 showed, in general, more potent antifungal activity than 6-arylthio-4,7-dioxobenzothiazoles 3 and 4. The 6-arylamino-substituted compounds 5 and 6 exhibited the greatest activity. In contrast, 6-arylthio-, 2-/5-methyl- or 5-methoxy-moieties of compounds 3-4 did not improve their antifungal activity significantly. The results of this study suggest that 6-arylamino-4,7-dioxobenzothiazoles would be potent antifungal agents.
Ryu
Chung Kyu
CK
College of Pharmacy, Ewha Womans University, Seodaemun-ku, Seoul 120-750, South Korea. cryu@mm.ewha.ac.kr
Choi
Ko Un
KU
Shim
Ju Yeon
JY
You
Hea Jung
HJ
Choi
Ik Hwa
IH
Chae
Mi Jin
MJ
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D013844:Thiazoles