Screening and Application of Chitin Synthase Inhibitors

被引：6

作者：

Shi, Xiaozai ^{[1
]}

Qiu, Shuo ^{[1
]}

Bao, Yingling ^{[1
]}

Chen, Hanchi ^{[1
]}

Lu, Yuele ^{[1
]}

Chen, Xiaolong ^{[1
]}

机构：

[1] Zhejiang Univ Technol, Coll Biotechnol & Bioengn, Hangzhou 310014, Peoples R China

来源：

PROCESSES | 2020年 / 8卷 / 09期

基金：

中国国家自然科学基金;

关键词：

chitin synthase; maleimides; inhibitors; biological activity research; ANTIFUNGAL ACTIVITY; MALEIC-ANHYDRIDE; TAUTOMYCIN;

D O I：

10.3390/pr8091029

中图分类号：

TQ [化学工业];

学科分类号：

0817 ;

摘要：

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half-inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

引用

页数：12

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