DESIGN, SYNTHESIS, AND FUNGICIDAL ACTIVITY EVALUATION OF 2-METHYL-5-PHENYLTHIAZOLE-4-CARBOXAMIDES BEARING MORPHOLINE, THIOMORPHOLINE, OR THIOMORPHOLINE 1,1-DIOXIDE MOIETY

Авторы

  • Jimin Wei School of Pharmacy, Shenzhen University Medical School, 3688 Nanhai Road, Nanshan District, Shenzhen 518055
  • Lili Chen School of Pharmacy, Shenzhen University Medical School, 3688 Nanhai Road, Nanshan District, Shenzhen 518055
  • Kunfang Zhu School of Pharmacy, Shenzhen University Medical School, 3688 Nanhai Road, Nanshan District, Shenzhen 518055
  • Yong-Xian Cheng School of Pharmacy, Shenzhen University Medical School, 3688 Nanhai Road, Nanshan District, Shenzhen 518055
  • Danling Huang School of Pharmacy, Shenzhen University Medical School, 3688 Nanhai Road, Nanshan District, Shenzhen 518055

Ключевые слова:

morpholine derivatives, thiazole derivatives, thiomorpholine derivatives, fungicidal activity, structural optimization, structure– activity relationship

Аннотация

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-(trifluoromethyl)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.

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Опубликован

2024-12-13

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Раздел

Оригинальные статьи