Abstract <p>A series of novel <i>N</i>-(2-aryl/arylmethylaminoethyl)-1,4-benzoxazines was designed, synthesized, and evaluated for their antifungal activities against six phytopathogenic fungi. The bioassay results showed that the compounds exhibited good to excellent activity. Among them, <i>N</i>-[2-(3-chlorophenylamino)ethyl]-3,4-dihydro-2<i>H</i>-1,4-benzoxazine showed the highest potency of 95.2% inhibitory activity against <i>S. sclerotiorum.</i> Furthermore, molecular docking studies suggested that succinate dehydrogenase (SDH) may serve as a potential target for these compounds.</p>

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Synthesis, Antifungal Activity and Molecular Docking Studies of Novel N-(2-Aryl/arylmethylaminoethyl)-1,4-benzoxazine Derivatives

  • Zilong Tang,
  • Zihao Wu,
  • Meiyan Cui,
  • Yuhuan Tan,
  • Xiaoling Ou,
  • Qianyi He,
  • Ziyue Jiang

摘要

Abstract

A series of novel N-(2-aryl/arylmethylaminoethyl)-1,4-benzoxazines was designed, synthesized, and evaluated for their antifungal activities against six phytopathogenic fungi. The bioassay results showed that the compounds exhibited good to excellent activity. Among them, N-[2-(3-chlorophenylamino)ethyl]-3,4-dihydro-2H-1,4-benzoxazine showed the highest potency of 95.2% inhibitory activity against S. sclerotiorum. Furthermore, molecular docking studies suggested that succinate dehydrogenase (SDH) may serve as a potential target for these compounds.