title: [Synthesis and antifungal activity of novel triazole antifungal agents].
abstract: OBJECTIVE
  A series of triazole antifungal agents were synthesized to search for novel triazole antifungal agents with more potent activity, less toxicity and broader spectrum.
  
  
  METHODS
  Twenty-one 1-(1H-1, 2, 4-triazolyl)-2-(2, 4-diflurophenyl)-3-(4-substituted-1-piperazinyl)-2-propanols were synthesized, on the basis of the three dimensional structure of P450 cytochrome 14alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.
  
  
  RESULTS
  Results of preliminary biological tests showed that most of title compounds exhibited activity against the eight common pathogenic fungi to some extent and the activities against deep fungi were higher than that against shallow fungi. In general, phenyl and pyridinyl analogues showed higher antifungal activity than that of the phenylacyl analogues.
  
  
  CONCLUSIONS
  Several title compounds showed higher antifungal activities than fluconazole and terbinafine. Compound VIII-1, 4, 5 and IX-3 showed the best antifungal activity with broad antifungal spectrum and were chosen for further study.
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: Jie
authors.initials: J
authors.lastname: Zhu
authors.forename: Wan-nian
authors.initials: WN
authors.lastname: Zhang
authors.forename: Yun-long
authors.initials: YL
authors.lastname: Song
authors.forename: Min
authors.initials: M
authors.lastname: Zhang
authors.forename: Hai-tao
authors.initials: HT
authors.lastname: Ji
authors.forename: Jian-xin
authors.initials: JX
authors.lastname: Yu
authors.forename: Jian-zhong
authors.initials: JZ
authors.lastname: Yao
authors.forename: Song
authors.initials: S
authors.lastname: Yang
authors.forename: Zhen-yuan
authors.initials: ZY
authors.lastname: Miao
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; D015725:Fluconazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009281:Naphthalenes / Q000494:pharmacology; D013329:Structure-Activity Relationship; D000077291:Terbinafine; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D009281:Naphthalenes; D014230:Triazoles; D015725:Fluconazole; D000077291:Terbinafine