Screening and Application of Chitin Synthase Inhibitors

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 inh...

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Main Authors:	Xiaozai Shi, Shuo Qiu, Yingling Bao, Hanchi Chen, Yuele Lu, Xiaolong Chen
Format:	Article
Language:	English
Published:	MDPI AG 2020-08-01
Series:	Processes
Subjects:	chitin synthase maleimides inhibitors biological activity research
Online Access:	https://www.mdpi.com/2227-9717/8/9/1029

id	doaj-0fa36950764b48a2aa4696eff9aec557
record_format	Article
spelling	doaj-0fa36950764b48a2aa4696eff9aec5572020-11-25T02:58:47ZengMDPI AGProcesses2227-97172020-08-0181029102910.3390/pr8091029Screening and Application of Chitin Synthase InhibitorsXiaozai Shi0Shuo Qiu1Yingling Bao2Hanchi Chen3Yuele Lu4Xiaolong Chen5College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaCollege of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, ChinaChitin 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 (IC<sub>50</sub>) value of compound <b>20</b> on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC<sub>50</sub> = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.https://www.mdpi.com/2227-9717/8/9/1029chitin synthasemaleimidesinhibitorsbiological activity research
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Xiaozai Shi Shuo Qiu Yingling Bao Hanchi Chen Yuele Lu Xiaolong Chen
spellingShingle	Xiaozai Shi Shuo Qiu Yingling Bao Hanchi Chen Yuele Lu Xiaolong Chen Screening and Application of Chitin Synthase Inhibitors Processes chitin synthase maleimides inhibitors biological activity research
author_facet	Xiaozai Shi Shuo Qiu Yingling Bao Hanchi Chen Yuele Lu Xiaolong Chen
author_sort	Xiaozai Shi
title	Screening and Application of Chitin Synthase Inhibitors
title_short	Screening and Application of Chitin Synthase Inhibitors
title_full	Screening and Application of Chitin Synthase Inhibitors
title_fullStr	Screening and Application of Chitin Synthase Inhibitors
title_full_unstemmed	Screening and Application of Chitin Synthase Inhibitors
title_sort	screening and application of chitin synthase inhibitors
publisher	MDPI AG
series	Processes
issn	2227-9717
publishDate	2020-08-01
description	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 (IC<sub>50</sub>) value of compound <b>20</b> on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC<sub>50</sub> = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.
topic	chitin synthase maleimides inhibitors biological activity research
url	https://www.mdpi.com/2227-9717/8/9/1029
work_keys_str_mv	AT xiaozaishi screeningandapplicationofchitinsynthaseinhibitors AT shuoqiu screeningandapplicationofchitinsynthaseinhibitors AT yinglingbao screeningandapplicationofchitinsynthaseinhibitors AT hanchichen screeningandapplicationofchitinsynthaseinhibitors AT yuelelu screeningandapplicationofchitinsynthaseinhibitors AT xiaolongchen screeningandapplicationofchitinsynthaseinhibitors
_version_	1724705159941980160

Screening and Application of Chitin Synthase Inhibitors

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