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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.