NDLI: Discovery and SAR study of piperidine-based derivatives as novel influenza virus inhibitors

Content Provider	PubMed Central
Author	Wang, Guoxin Chen, Longjian Xian, Tongmei Liang, Yujie Zhang, Xintao Yang, Zhen Luo, Ming
Abstract	A series of piperidine-based derivatives were identified as novel and potent inhibitors of influenza virus through structural modification of the original compound that was selected from a high-throughput screen. Various analogues were synthesized and confirmed as inhibitors. The structure-activity relationship (SAR) studies suggested that the ether linkage between the quinoline and piperidine is critical to the inhibitory activity. Optimized compoundtert-Butyl 4-(quinolin-4-yloxy)piperidine-1-carboxylate11ehad an excellent inhibitory activity of influenza virus infection against a variety of influenza virus strains with EC50 values as low as 0.05 μM. The selectivity index value (SI = MLD50/EC50) of 11e is over 160,000 based on cytotoxicity measured by MTT assays of three cell lines. We carried out the time-of-addition experiment to delineate the mechanism of inhibition. The result indicates that 11e interferes with an early to middle stage of influenza virus replication.
Related Links	http://dx.doi.org/10.1039/c4ob01079e
Ending Page	8060
Page Count	13
Starting Page	8048
File Format	PDF
ISSN	14770520
e-ISSN	14770539
Journal	Organic & biomolecular chemistry
Issue Number	40
Volume Number	12
Language	English
Publisher Date	2014-08-01
Access Restriction	Open
Subject Keyword	Physical and Theoretical Chemistry Organic Chemistry Biochemistry Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry Physical and Theoretical Chemistry

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