title: Synthesis and antifungal activity of novel triazole derivatives.
abstract: A series of novel azoles (a-v), which are analogues of fluconazole, have been designed and synthesized as potential antifungal agents by the click reaction. The click reaction approach toward the synthesis of novel 1,2,3-triazolyl linked triazole antifungal derivatives a-v was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of propargylated intermediate 5 with substituted azidomethyl benzene. In addition, the target compounds tested can increase antifungal activity.
authors.affiliation: Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Guohe Road 325, Shanghai 200433, China.
authors.forename: Yongzheng
authors.initials: Y
authors.lastname: Yan
authors.forename: Shichong
authors.initials: S
authors.lastname: Yu
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Chai
authors.forename: Honggang
authors.initials: H
authors.lastname: Hu
authors.forename: Qiuye
authors.initials: Q
authors.lastname: Wu
mesh_terms: D058888:14-alpha Demethylase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002384:Catalysis; D003300:Copper; D005658:Fungi / Q000187:drug effects / Q000201:enzymology; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D058888:14-alpha Demethylase Inhibitors; D000935:Antifungal Agents; D007202:Indicators and Reagents; D014230:Triazoles; D003300:Copper