title: 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.
abstract: 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.
authors.affiliation: School of Pharmacy, Second Military Medical University, P. R. China.
authors.forename: Ping-Hui
authors.initials: PH
authors.lastname: Gao
authors.forename: Yong-Bing
authors.initials: YB
authors.lastname: Cao
authors.forename: Zheng
authors.initials: Z
authors.lastname: Xu
authors.forename: Jun-Dong
authors.initials: JD
authors.lastname: Zhang
authors.forename: Wan-Nian
authors.initials: WN
authors.lastname: Zhang
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Jun
authors.initials: J
authors.lastname: Gu
authors.forename: Ying-Ying
authors.initials: YY
authors.lastname: Cao
authors.forename: Ruo-Yu
authors.initials: RY
authors.lastname: Li
authors.forename: Xin-Ming
authors.initials: XM
authors.lastname: Jia
authors.forename: Yuan-Ying
authors.initials: YY
authors.lastname: Jiang
mesh_terms: 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*
chemical_list: D000935:Antifungal Agents; D001596:Benzylamines; D009281:Naphthalenes; D014230:Triazoles; C505685:ZJ-522; D015725:Fluconazole; C067594:butenafine