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Diversity-oriented synthesis of marine polybrominated diphenyl ethers as potential KCNQ potassium channel activators

文献类型：期刊论文

作者Liu, Lai-Xin1,2; Gu, Ru-Rong1,3; Jin, Yang1,2; Chen, Xue-Qin3; Li, Xu-Wen1,2,4; Zheng, Yue-Ming3; Gao, Zhao-Bing3,5; Guo, Yue-Wei1,2,4
刊名BIOORGANIC CHEMISTRY
出版日期2022-09
卷号126页码:105909
关键词Marine Natural product Polybrominated diphenyl ethers KCNQ potassium channel
ISSN号0045-2068
DOI10.1016/j.bioorg.2022.105909
文献子类Article
英文摘要Natural polybrominated diphenyl ethers, often isolated from marine sponges, have been reported to possess various biological activities, such as antibacterial, antioxidant and antidiabetic effects. Via a high throughput screening of our marine natural product library, the polybrominated diphenyl ether 3 was found to display a KCNQ potassium channel activation effect. To obtain more compound 3 related natural products and their derivatives for further bioactivity study, a diversity-oriented synthesis was conducted, leading to the successful synthesis of five polybrominated diphenyl ether natural products (1-4, 6) and 30 new derivatives. Compound 3 was found to preferentially potentiate KCNQ1 potassium channel, whereas 17h relatively activated KCNQ2 potassium channel. The structure-activity relationship was analyzed assisted by molecular docking and 17h was further conducted for its agonistic mechanism study on KCNQ2 channel. This research work may give an insight for the discovery of marine polybrominated diphenyl ether derived new drug leads.
WOS关键词DYSIDEA-HERBACEA ; RETIGABINE ; DISCOVERY ; DERIVATIVES
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000823365000001
出版者ACADEMIC PRESS INC ELSEVIER SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/309342]  
专题新药研究国家重点实验室
通讯作者Zheng, Yue-Ming; Gao, Zhao-Bing; Guo, Yue-Wei
作者单位1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Neurol & Psychiat Res & Drug Discovery, Shanghai 201203, Peoples R China;
4.Bohai Rim Adv Res Inst Drug Discovery, Drug Discovery Shandong Lab, Yantai 264117, Shandong, Peoples R China;
5.Chinese Acad Sci, Inst Drug Discovery Innovat, Zhongshan Inst Drug Discovery, Zhongshan 528400, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Lai-Xin,Gu, Ru-Rong,Jin, Yang,et al. Diversity-oriented synthesis of marine polybrominated diphenyl ethers as potential KCNQ potassium channel activators[J]. BIOORGANIC CHEMISTRY,2022,126:105909.
APA Liu, Lai-Xin.,Gu, Ru-Rong.,Jin, Yang.,Chen, Xue-Qin.,Li, Xu-Wen.,...&Guo, Yue-Wei.(2022).Diversity-oriented synthesis of marine polybrominated diphenyl ethers as potential KCNQ potassium channel activators.BIOORGANIC CHEMISTRY,126,105909.
MLA Liu, Lai-Xin,et al."Diversity-oriented synthesis of marine polybrominated diphenyl ethers as potential KCNQ potassium channel activators".BIOORGANIC CHEMISTRY 126(2022):105909.

入库方式： OAI收割

来源：上海药物研究所

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