title: [Synthesis and antifungal activity of 1-(1,2,4-triazolyl-1H-1-yl)-2-(2,4-diflurophenyl)-3-(4-substituted benzyl-1-piperazinyl)-2-propanols].
abstract: OBJECTIVE
  A series of triazole antifungals were synthesized to search for novel triazole antifungals with more potent activity, less toxicity and broader spectrum.
  
  
  METHODS
  Nineteen 1-(1,2,4-triazolyl-1H-1-yl)-2-(2,4-diflurophenyl)-3-(4-substituted benzyl-1-piperazinyl)-2-propanols were designed and synthesized, on basis of the three dimensional structure of P450 cytochrome 14 alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.
  
  
  RESULTS
  All the title compounds were first reported. Results of preliminary biological tests showed that most of the title compounds exhibited high activity against the eight common pathogenic fungi and the activities against deep fungi were higher than that against shallow fungi.
  
  
  CONCLUSIONS
  Most of the title compounds showed higher antifungal activities than Fluconazole and Terbinafine. Compound VIII-1, 10, 12, 17 showed best antifungal activity with broad antifungal spectrum and were chosen for further development.
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai, 200433, China.
authors.forename: Chun-quan
authors.initials: CQ
authors.lastname: Sheng
authors.forename: Wan-nian
authors.initials: WN
authors.lastname: Zhang
authors.forename: Hai-tao
authors.initials: HT
authors.lastname: Ji
authors.forename: Yun-long
authors.initials: YL
authors.lastname: Song
authors.forename: Song
authors.initials: S
authors.lastname: Yang
authors.forename: You-jun
authors.initials: YJ
authors.lastname: Zhou
authors.forename: Ju
authors.initials: J
authors.lastname: Zhu
authors.forename: Jia-guo
authors.initials: JG
authors.lastname: Lü
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D003455:Cryptococcus neoformans / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D014230:Triazoles