Synthesis and evaluation of quinoxaline derivatives as potential influenza NS1A protein inhibitors
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.
You, Lei,Cho, Eun Jeong,Leavitt, John,Ma, Li-Chung,Montelione, Gaetano T.,Anslyn, Eric V.,Krug, Robert M.,Ellington, Andrew,Robertus, Jon D.
supporting information; experimental part
p. 3007 - 3011
(2011/06/24)
Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors
From chemical compound library screening using an HCV NS5B RNA-dependent RNA polymerase enzymatic assay, we identified a substituted quinoxaline hit with an IC50 of 5.5 μM. A series of substituted quinoxaline amide derivatives were synthesized
Rong, Frank,Chow, Suetying,Yan, Shunqi,Larson, Gary,Hong, Zhi,Wu, Jim
p. 1663 - 1666
(2008/02/13)
Substituted 5- and 6-quinoxalinecarboxylic acids and their tuberculostatic activity
-
Roubinek,Bydzovsky,Budesinsky
p. 285 - 294
(2007/10/02)
More Articles about upstream products of 90833-63-9