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Design, synthesis and biological evaluation of novel inhibitors against cyanobacterial pyruvate dehydrogenase multienzyme complex E1

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成果类型:
期刊论文
作者:
Feng, Jiangtao;He, Haifeng;Zhou, Yuan;Guo, Xiaoliang;Liu, Honglin;...
通讯作者:
Feng, Lingling(冯玲玲);He, Hongwu
作者机构:
[Feng, Lingling; He, Hongwu; He, HW; Feng, Jiangtao; He, Haifeng; Cai, Meng; Liu, Honglin; Guo, Xiaoliang; Wang, Fang; Zhou, Yuan] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Hubei, Peoples R China.
[He, Haifeng] Jiangxi Sci & Technol Normal Univ, Sch Chem & Chem Engn, Nanchang 330013, Jiangxi, Peoples R China.
通讯机构:
[Feng, LL; He, HW] C
Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Hubei, Peoples R China.
语种:
英文
关键词:
Algicide;Cyanobacterial blooms;Inhibitor;Pyruvate dehydrogenase multienzyme component E1;Thiamin diphosphate (ThDP) analogs
期刊:
Bioorganic & Medicinal Chemistry
ISSN:
0968-0896
年:
2019
卷:
27
期:
12
页码:
2413-2420
基金类别:
The work was supported by National Research and Development Plan (No. 2017YFD0200506), the Natural Science Foundation of China (No. 21877047 , 21472062 , 21877046 , 21867011 , 21472061 and 31701820 ), and the Project of the Science Fund of Jiangxi Education Office (GJJ170672), the Project of Hubei Natural Science Foundation (2017CFB232), China postdoctoral science foundation (2017M622486). The work was also financially supported by self-determined research funds of CCNU from the colleges’ basic research and operation of MOE (CCNU18ZDPY02) and the Program of Introducing Talents of Discipline to Universities of China (111 program, B17019).
机构署名:
本校为第一且通讯机构
院系归属:
化学学院
摘要:
Cyanobacterial pyruvate dehydrogenase multienzyme complex E1 (PDHc E1)is a potential target enzyme for finding inhibitors to control harmful cyanobacterial blooms. In this study, a series of novel triazole thiamin diphosphate (ThDP)analogs were designed and synthesized by modifying the substituent group of triazole ring and optimizing triazole-benzene linker as potential cyanobacterial PDHc E1 (Cy-PDHc E1)inhibitors. Their inhibitory activities against Cy-PDHc E1 in vitro and algicide activities in vivo were further examined. Most of these comp...

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