Article
Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity.
European journal of medicinal chemistry - 25 Mar 2018
Liu Baomin, Gai Kuo, Qin Hui, Liu Xushi, Cao Yuan, Lu Qin, Lu Dandan, Chen Deyang, Shen Hengqiao, Song Wei, Zhang Yang, Wang Xiaojin, Xu Hongjiang, Zhang Yinsheng
Abstract excerpt
Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV genotypes (GT 1 to 6) of 10d is increased to some extent, especially the inhibitory activity...
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