title: Synthesis and Antifungal Activity of Novel Myrtenal-Based 4-Methyl-1,2,4-triazole-thioethers.
abstract: A series of novel myrtenal derivatives bearing 1,2,4-triazole moiety were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Their structures were confirmed by using UV-vis, FTIR, NMR, and ESI-MS analysis. Antifungal activity of the target compounds was preliminarily evaluated by the in vitro method againstFusarium oxysporumf. sp.cucumerinum,Physalospora piricola,Alternaria solani,Cercospora arachidicola, andGibberella zeaeat 50 µg/mL. Compounds6c(R =i-Pr),6l(R =o-NO₂ Bn), and6a(R = Et) exhibited excellent antifungal activity againstP. piricolawith inhibition rates of 98.2%, 96.4%, and 90.7%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide azoxystrobin with a 96.0% inhibition rate, which served as a positive control.
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, Guangxi, China. gxlinguas@sina.com.
authors.forename: Gui-Shan
authors.initials: GS
authors.lastname: Lin
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, Guangxi, China. wgduan@gxu.edu.cn.
authors.forename: Wen-Gui
authors.initials: WG
authors.lastname: Duan
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, Guangxi, China. gslin@gxu.edu.cn.
authors.forename: Lin-Xiao
authors.initials: LX
authors.lastname: Yang
authors.affiliation: School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, Guangxi, China. gaominhuang@mail.gxu.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Huang
authors.affiliation: Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Nanning 530008, Guangxi, China. dwg105@gxu.edu.cn.
authors.forename: Fu-Hou
authors.initials: FH
authors.lastname: Lei
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000081008:Bicyclic Monoterpenes; D002849:Chromatography, Gas; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013440:Sulfides / Q000737:chemistry; D013729:Terpenes / Q000737:chemistry; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D000081008:Bicyclic Monoterpenes; D013440:Sulfides; D013729:Terpenes; D014230:Triazoles; C045575:1,2,4-triazole; C061545:myrtenal
keywords: 1,2,4-triazole-thioether; antifungal activity; myrtenal; α-pinene