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
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.