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Discovery of Novel Oxathiapiprolin Derivatives as Potent Fungicide Candidates

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成果类型:
期刊论文
作者:
Zhou, Li-Ming;Yang, Jing-Fang;Li, Hong-Hao;Chen, Wei;Li, Yi-Wen;...
通讯作者:
Zhu, Xiao-Lei;Yang, GF
作者机构:
[Yang, Jing-Fang; Chen, Wei; Zhu, Xiao-Lei; Zhu, XL; Li, Yi-Wen; Yang, Guang-Fu; Yang, GF; Li, Hong-Hao; Zhou, Li-Ming] Cent China Normal Univ, Int Joint Res Ctr Intelligent Biosensor Technol &, Minist Sci & Technol, State Key Lab Green Pesticide,Key Lab Pesticide &, Wuhan 430079, Peoples R China.
[Yang, Guang-Fu; Yang, GF] Collaborat Innovat Ctr Chem Sci & Engn, Tianjin 300071, Peoples R China.
通讯机构:
[Zhu, XL; Yang, GF ] C
Cent China Normal Univ, Int Joint Res Ctr Intelligent Biosensor Technol &, Minist Sci & Technol, State Key Lab Green Pesticide,Key Lab Pesticide &, Wuhan 430079, Peoples R China.
Collaborat Innovat Ctr Chem Sci & Engn, Tianjin 300071, Peoples R China.
语种:
英文
关键词:
indole;oxathiapiprolin;substituent optimization;oxysterol-binding protein inhibitor;fungicide;interaction mechanism
期刊:
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
ISSN:
0021-8561
年:
2024
卷:
72
期:
31
页码:
17649-17657
基金类别:
National Key Research and Development Program of China [2022YFD1700204]; National Natural Science Foundation of China [21977035]
机构署名:
本校为第一且通讯机构
院系归属:
化学学院
摘要:
Oxathiapiprolin (OXA), which targets the oxysterol-binding protein (OSBP), is an outstanding piperidinyl thiazole isoxazoline (PTI) fungicide that can be used to control oomycetes diseases. In this study, starting from the structure of OXA, a series of novel OSBP inhibitors were designed and synthesized by introducing an indole moiety to replace the pyrazole in OXA. Finally, compound b24 was found to exhibit the highest control effect (82%) against cucumber downy mildew (CDM) in the greenhouse at a very low dosage of 0.069 mg/L, which was comparable to that of OXA (88%). Furthermore, it showed...

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