title: Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents.
abstract: A series of 1-(substituted biaryloxy)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl) propan-2-ol were synthesized and their antifungal activities were evaluated against eight human pathogenic fungi in vitro. Seventeen compounds showed activity 4- to 64-fold higher than voriconazole against Candida albicans. SAR clearly suggested that introduction of a biaryloxy side chain greatly enhanced the antifungal activity of triazole analogs against Candida species.
authors.affiliation: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
authors.forename: Ping
authors.initials: P
authors.lastname: Liu
authors.forename: Shaolong
authors.initials: S
authors.lastname: Zhu
authors.forename: Peng
authors.initials: P
authors.lastname: Li
authors.forename: Weijie
authors.initials: W
authors.lastname: Xie
authors.forename: Yongsheng
authors.initials: Y
authors.lastname: Jin
authors.forename: Qingyan
authors.initials: Q
authors.lastname: Sun
authors.forename: Qiuye
authors.initials: Q
authors.lastname: Wu
authors.forename: Peng
authors.initials: P
authors.lastname: Sun
authors.forename: Yingjun
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Yang
authors.forename: Yuanying
authors.initials: Y
authors.lastname: Jiang
authors.forename: Dazhi
authors.initials: D
authors.lastname: Zhang
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D015725:Fluconazole / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D065819:Voriconazole; D015003:Yeasts / Q000187:drug effects
chemical_list: D000935:Antifungal Agents; D011743:Pyrimidines; D014230:Triazoles; D015725:Fluconazole; D065819:Voriconazole