title: Synthesis and antifungal activity of the novel triazole derivatives containing 1,2,3-triazole fragment.
abstract: A series of fluconazole analogues containing 1,2,3-triazole fragment have been designed and synthesized on the basis of the active site of the cytochrome P450 14α-demethylase (CYP51). Their structures were characterized by (1)H NMR, (13)C NMR and LC-MS. The MIC80 values indicate that the target compounds 1a-r showed higher activities against nearly all the fungi tested to some extent except against Aspergillus fumigatus. Compounds 1c, e, f, l and p showed 128 times higher activity (with the MIC80 value of 0.0039 mg/mL) than that of fluconazole against Candida albicans and also showed higher activity than that of the other positive controls.
authors: Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai, 200433, People's Republic of China.
authors: Shichong
authors: S
authors: Yu
authors: Nan
authors: N
authors: Wang
authors: Xiaoyun
authors: X
authors: Chai
authors: Baogang
authors: B
authors: Wang
authors: Hong
authors: H
authors: Cui
authors: Qingjie
authors: Q
authors: Zhao
authors: Yan
authors: Y
authors: Zou
authors: Qingyan
authors: Q
authors: Sun
authors: Qingguo
authors: Q
authors: Meng
authors: Qiuye
authors: Q
authors: Wu
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015725:Fluconazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D014230:Triazoles; D015725:Fluconazole