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Design, synthesis, and fungicidal activity evaluation of 2-methyl-5-phenylthiazole-4-carboxamides bearing morpholine, thiomorpholine, or thiomorpholine 1,1-dioxide moiety

  • Jimin Wei,
  • Lili Chen,
  • Kunfang Zhu,
  • Yong-Xian Cheng,
  • Danling Huang

摘要

A series of 2-methyl-5-phenylthiazole derivatives were designed, synthesized, and characterized by 1H, 13C NMR spectra and HRMS. Subsequently, their antifungal activity was evaluated, and the bioassay results showed that almost all title compounds possess potential fungicidal activity against B. cinerea. [5-(4-Chlorophenyl)-2-methylthiazol-4-yl](morpholin-4-yl)methanone and {2-methyl-5-[4-(tri-fluoromethyl)phenyl]thiazol-4-yl}(thiomorpholin-4-yl)methanone displayed EC50 values of 19.6 mg/l and 15.6 mg/l respectively, against B. cinerea, showing higher potency than that of hymexazol.