Synthesis and evaluation of quinoxaline derivatives as potential influenza NS1A protein inhibitors

L You, EJ Cho, J Leavitt, LC Ma, GT Montelione…

文献索引：You, Lei; Cho, Eun Jeong; Leavitt, John; Ma, Li-Chung; Montelione, Gaetano T.; Anslyn, Eric V.; Krug, Robert M.; Ellington, Andrew; Robertus, Jon D. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 10 p. 3007 - 3011

全文：HTML全文

被引用次数: 33

摘要

Abstract A library of quinoxaline derivatives were prepared to target non-structural protein 1 of influenza A (NS1A) as a means to develop anti-influenza drug leads. An in vitro fluorescence polarization assay demonstrated that these compounds disrupted the dsRNA– NS1A interaction to varying extents. Changes of substituent at positions 2, 3 and 6 on the quinoxaline ring led to variance in responses. The most active compounds (35 and 44) ...