| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361947 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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) had IC50 values in the range of low micromolar concentration without exhibiting significant dsRNA intercalation. Compound 44 was able to inhibit influenza A/Udorn/72 virus growth.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Lei You, Eun Jeong Cho, John Leavitt, Li-Chung Ma, Gaetano T. Montelione, Eric V. Anslyn, Robert M. Krug, Andrew Ellington, Jon D. Robertus,