Structure optimization and bioactivity evaluation of ThDP analogs targeting cyanobacterial pyruvate dehydrogenase E1

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成果类型：

期刊论文

作者：

Feng, Jiangtao;He, Haifeng;Zhou, Yuan;Cai, Meng;Peng, Hao;...

通讯作者：

Feng, Lingling（冯玲玲）;He, Hongwu

作者机构：

[Feng, Lingling; He, Hongwu; Peng, Hao; He, HW; Feng, Jiangtao; He, Haifeng; Cai, Meng; Liu, Honglin; Zhou, Yuan; Liu, Lei] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Hubei, Peoples R China.

[Feng, Lingling; He, Hongwu; Peng, Hao; He, HW; Feng, Jiangtao; He, Haifeng; Cai, Meng; Liu, Honglin; Zhou, Yuan; Liu, Lei] Cent China Normal Univ, Coll Chem, 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, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Hubei, Peoples R China.

Cent China Normal Univ, Coll Chem, Wuhan 430079, Hubei, Peoples R China.

语种：

英文

关键词：

Algicides;Competitive inhibitors;Harmful cyanobacterial blooms;Pyruvate dehydrogenase multienzyme component E1;Thiamin diphosphate

期刊：

Bioorganic & Medicinal Chemistry

ISSN：

0968-0896

年：

2019

卷：

期：

页码：

115159

DOI：

10.1016/j.bmc.2019.115159

基金类别：

The work was supported by the Natural Science Foundation of China (No. 21877047 , 21877046 , 21867011 , 21472062 and 21472061 ), National Research and Development Plan (No. 2017YFD0200506 ), 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 ). Appendix A

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本校为第一且通讯机构

院系归属：

化学学院

摘要：

Harmful cyanobacteria bloom (HCB) has occurred frequently in recent years and it is urgent to develop novel algicides to deal with this problem. In this paper, a series of novel thiamin diphosphate (ThDP) analogs 5a-5g were designed and synthesized targeting cyanobacterial pyruvate dehydrogenase complex E1 (Cy-PDHc E1). Our results showed that compounds 5a-5g have higher inhibitory activities against Cy-PDHc E1 (IC50 9.56-3.48microM) and higher inhibitory activities against two model cyanobacteria strains Synechocystis sp PCC6803 (EC50 2.03-1.58microM) and Microcystis aeruginosa FACHB905 (EC50...

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Structure optimization and bioactivity evaluation of ThDP analogs targeting cyanobacterial pyruvate dehydrogenase E1

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