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Synthesis and Activity of 1,2,3-Triazole Aminopyrimidines against Cyanobacteria as PDHc-E1 Competitive Inhibitors.

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成果类型:
期刊论文
作者:
Zhou, Yuan;Feng, Jiangtao;Feng, Lingling(冯玲玲);Xie, Dan;Peng, Hao;...
通讯作者:
Cai, Meng;He, Hongwu
作者机构:
[Feng, Lingling; He, Hongwu; Peng, Hao; Cai, Meng; He, HW; Xie, Dan; Feng, Jiangtao; Zhou, Yuan] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, 152 Luoyu Rd, Wuhan 430079, Hubei, Peoples R China.
通讯机构:
[Cai, M; He, HW] C
Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, 152 Luoyu Rd, Wuhan 430079, Hubei, Peoples R China.
语种:
英文
关键词:
synthesis;PDHc-E1 inhibitor;anticyanobacteria;selectivity;molecular docking
期刊:
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
ISSN:
0021-8561
年:
2019
卷:
67
期:
45
页码:
12538-12546
基金类别:
National Research and Development Plan [2017YFD0200506]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China [21877047, 31701820, 21472062, 21907035]; 111 ProjectMinistry of Education, China - 111 Project [B17019]; Natural Science Foundation of Hubei Province of ChinaNatural Science Foundation of Hubei Province [2017CFB232]; National Key Research Development Program of China [2018YFD0200100]
机构署名:
本校为第一且通讯机构
院系归属:
化学学院
摘要:
Cyanobacteria harmful algal blooms are of global concern, but all currently available algicides in the market are nonselective and have potential side effects on nontarget species. In the present work, two series of compounds (4 and 6) comprising 16 novel 1,2,3-triazole aminopyrimidines were rationally designed and synthesized as control agent for cyanobacteria. Our design focus was the inhibiting cyanobacteria by inhibition against pyruvate dehydrogenase complex E1 (PDHc-E1). Compounds 4 and 6 showed potent inhibition against Escherichia coli PDHc-E1 (IC50 = 4.13-23.76 muM) and also strong al...

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