title: Synthesis and biological activity of novel 1-substituted phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-triazoles.
abstract: In an attempt to search for potent antifungal agents, a series of novel 1-substituted phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-triazoles 5a-m was designed and synthesized via Huisgen cycloaddition reaction between various (2-morpholinoethoxy)-N-(prop-2-ynyl)aniline and different azidobenzene. Their chemical structures were characterized by (1) H NMR and elemental analysis. A cleaner reaction with milder conditions and satisfactory yields was observed in the micorwave-assisted synthesis of 4a-c. The fungicidal activity of some target compounds were evaluated in vitro against Fusarium omysporum, Physalospora piricola, Alternaria solani, Cercospora arachidicola and Gibberella zeae at 50 μg/mL. The bioassay results indicated that some compounds exhibited moderate fungicidal activities. Furthermore, compound 5h displayed equal activity to the positive control compounds against Alternaria solani.
authors: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.
authors: Ming-Zhen
authors: MZ
authors: Mao
authors: Yu-Xin
authors: YX
authors: Li
authors: Yun-Yun
authors: YY
authors: Zhou
authors: Wei
authors: W
authors: Chen
authors: Tuan-Wei
authors: TW
authors: Liu
authors: Shu-Jing
authors: SJ
authors: Yu
authors: Su-Hua
authors: SH
authors: Wang
authors: Zheng-Ming
authors: ZM
authors: Li
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D005658:Fungi / Q000187:drug effects*; D006801:Humans; D009181:Mycoses / Q000188:drug therapy; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D014230:Triazoles