Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors

A series of 4-thiazolinone derivatives (D1-D58) were designed and synthesized. All of the derivatives were evaluated in vitro for neuraminidase (NA) inhibitory activities against influenza virus A (H1N1), and the inhibitory activities of the five most potent compounds were further evaluated on NA fr...

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Bibliographic Details
Published in:	European journal of medicinal chemistry 2021-03, Vol.213, p.113161, Article 113161
Main Authors:	Xiao, Mengwu, Xu, Lvjie, Lin, Ding, Lian, Wenwen, Cui, Manying, Zhang, Meng, Yan, Xiaowei, Li, Shuishi, Zhao, Jun, Ye, Jiao, Liu, Ailin, Hu, Aixi
Format:	Article
Language:	English
Subjects:	4-Thiazolinone derivatives Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Dose-Response Relationship, Drug Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Influenza Influenza A Virus, H3N2 Subtype - drug effects Influenza A Virus, H3N2 Subtype - enzymology Microbial Sensitivity Tests Molecular Docking Simulation Molecular Structure Neuraminidase - antagonists & inhibitors Neuraminidase - metabolism Neuraminidase inhibitors Structure-Activity Relationship Synthesis Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - pharmacology
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