4.6 Article

Design, Synthesis, and Anti-Fungal Evaluation of Heterocyclic Benzoxazole Derivatives

Journal

MOLECULES
Volume 27, Issue 23, Pages -

Publisher

MDPI
DOI: 10.3390/molecules27238375

Keywords

benzoxazole; crystal structure; synthesis; anti-fungal activities

Funding

  1. National Natural Science Foundation of China
  2. [20802058]

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A series of benzoxazole derivatives were synthesized and evaluated for their antifungal activity. Most of the compounds showed moderate antifungal activities, with three candidates exhibiting the strongest activity.
In order to discover more promising anti-fungal agents, a series of benzoxazole family was synthesized by PPA-catalyzed condensation and a Raney nickel/hydrazine reduction. Altogether 45 compounds were obtained in good to excellent yields and characterized by FT-IR, NMR, MS, and X-ray crystal diffraction. Moreover, the biological activity against eight phytopathogenic fungi was investigated. All in all, most of these compounds bear moderate antifungal activities. Among them, three candidates show the strongest activities, compound 4ac, 4bc provided over 50% inhibition rate against five fungi. Especially, the inhibitory rate of compound 4ah on Mycosphaerella melonis reached 76.4%.

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