In vitro antifungal activity of ZJ-522, a new triazole restructured from fluconazole and butenafine, against clinically important fungi in comparison with fluconazole and butenafine.
The antifungal activity of ZJ-522, a new triazole antifungal agent restructured from fluconazole and butenafine, was compared to that of fluconazole and butenafine against 43 strains of fungi representing 13 fungal species. MICs were determined by using the National Committee for Clinical Laboratory Standards (NCCLS)-recommended broth microdilution method for yeasts, which was modified for filamentous fungi. ZJ-522 was about 50-fold and 2 to 16-fold more potent than fluconazole against yeasts and filamentous fungi respectively, but it was less active than butenafine against filamentous fungi, although butenafine was inactive against most yeasts. Thus, the fashion of ZJ-522 antifungal activity more similar to that of fluconazole than that of butenafine indicates that ZJ-522 should be an inhibitor of lanosterol 14alpha-demethylase but not of squalene epoxidase, and should be a candidate for clinical development.
Gao
Ping-Hui
PH
School of Pharmacy, Second Military Medical University, P. R. China.
Cao
Yong-Bing
YB
Xu
Zheng
Z
Zhang
Jun-Dong
JD
Zhang
Wan-Nian
WN
Wang
Yan
Y
Gu
Jun
J
Cao
Ying-Ying
YY
Li
Ruo-Yu
RY
Jia
Xin-Ming
XM
Jiang
Yuan-Ying
YY
D000935:Antifungal Agents / Q000494:pharmacology*; D001596:Benzylamines / Q000737:chemistry* / Q000494:pharmacology; D015725:Fluconazole / Q000737:chemistry* / Q000494:pharmacology; D005658:Fungi / Q000145:classification / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009281:Naphthalenes / Q000737:chemistry* / Q000494:pharmacology; D014230:Triazoles / Q000494:pharmacology*
D000935:Antifungal Agents; D001596:Benzylamines; D009281:Naphthalenes; D014230:Triazoles; C505685:ZJ-522; D015725:Fluconazole; C067594:butenafine