标题:Synthesis and Preliminary Biologic Evaluation of 5-Substituted-2-(4-substituted phenyl)-1,3-Benzoxazoles as A Novel Class of Influenza Virus A Inhibitors
作者:Li, Zhenyu; Zhan, Peng; Naesens, Lieve; Vanderlinden, Evelien; Liu, Ailin; Du, Guanhua; De Clercq, Erik; Liu, Xinyong
作者机构:[Li, Zhenyu; Zhan, Peng; Liu, Xinyong] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Jinan 250012, Shandong, Peoples R China.; [Naesens, Lieve; 更多
通讯作者:Liu, XY
通讯作者地址:[Liu, XY]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, 44 W Culture Rd, Jinan 250012, Shandong, Peoples R China.
来源:CHEMICAL BIOLOGY & DRUG DESIGN
出版年:2012
卷:79
期:6
页码:1018-1024
DOI:10.1111/j.1747-0285.2012.01344.x
关键词:anti-influenza agents; antiviral activity; benzoxazoles; influenza A;; influenza virus
摘要:The diversity-oriented chemistry synthesis together with the random screening approach has permitted the discovery and optimization of novel antiviral lead compounds. In this paper, a series of novel 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles was synthesized and evaluated for their in vitro anti-influenza A virus and anti-influenza B virus activity. The activity was monitored by the MTS assay in the MadinDarby canine kidney cells. Compound 7h showed excellent inhibitory activity and selective index against A/H3N2 (EC50 = 37.03 mu m, SI > 5), which were all higher than that of the reference drug oseltamivir (EC50 > 59.00 mu m, SI > 1). However, no compound displays inhibitory activity against influenza B virus.
收录类别:SCOPUS;SCIE
WOS核心被引频次:2
Scopus被引频次:2
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84862820160&doi=10.1111%2fj.1747-0285.2012.01344.x&partnerID=40&md5=d18451a4b46db9fbde9a1a3ab643f3a7
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