Natural Product‐Based Fungicides Discovery: Design, Synthesis and Antifungal Activities of Some Sarisan Analogs Containing 1,3,4‐Oxadiazole Moieties | Zendy

Xu Hongyu | Zendy; Jia Ao | Zendy; Hou Enhua | Zendy; Liu Zhiyan | Zendy; Yang Rui | Zendy; Yang Ruige | Zendy; Guo Yong | Zendy

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Natural Product‐Based Fungicides Discovery: Design, Synthesis and Antifungal Activities of Some Sarisan Analogs Containing 1,3,4‐Oxadiazole Moieties

Author(s) -

Xu Hongyu,

Jia Ao,

Hou Enhua,

Liu Zhiyan,

Yang Rui,

Yang Ruige,

Guo Yong

Publication year - 2020

Publication title -

chemistry and biodiversity

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.427

H-Index - 70

eISSN - 1612-1880

pISSN - 1612-1872

DOI - 10.1002/cbdv.201900570

Subject(s) - fungicide , natural product , antifungal , chemistry , fusarium , alternaria solani , fusarium solani , oxadiazole , in vitro , stereochemistry , organic chemistry , microbiology and biotechnology , biology , botany , biochemistry

A series of sarisan analogs containing 1,3,4‐oxadiazole moieties were synthesized by iodine‐mediated oxidative cyclization and screened in vitro for their antifungal activities at 50 μg/mL against five phytopathogenic fungi such as Valsa mali , Curvularia lunata , Alternaria alternate , Fusarium solani and Fusarium graminearum . 1,3,4‐Oxadiazole derivatives 7e , 7p , 7r , 7t and 7u exhibited potent and a broad spectrum of antifungal activities against at least three phytopathogenic fungi at the concentration of 50 μg/mL. Especially, compound 7r displayed more potent antifungal activities against five phytopathogenic fungi than the positive control hymexazol. The EC 50 of 7r against V. mali , C. lunata and A. alternate were 12.6, 14.5 and 17.0 μg/mL, respectively. Additionally, some interesting results of structure‐activity relationships (SARs) were also observed.

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