Bioorganic & medicinal chemistry

Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases

C Nitsche, C Steuer, CD Klein

文献索引：Nitsche, Christoph; Steuer, Christian; Klein, Christian D. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 24 p. 7318 - 7337

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被引用次数: 51

摘要

The 3-aryl-2-cyanoacrylamide scaffold was designed as core pharmacophore for inhibitors of the Dengue and West Nile virus serine proteases (NS2B-NS3). A total of 86 analogs was prepared to study the structure–activity relationships in detail. Thereby, it turned out that the electron density of the aryl moiety and the central double bond have a crucial influence on the activity of the compounds, whereas the influence of substituents of the amide residue ...