94937-86-7Relevant articles and documents
Imidazo[4,5-c]pyridine derivative and application thereof
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, (2019/10/01)
The invention relates to a novel imidazo[4,5-c]pyridine derivative represented by a general formula I, and pharmaceutically acceptable salts, solvates or prodrugs of the novel imidazo[4,5-c]pyridine derivative, wherein the substituent R and R' are defined as in the specification. The invention also relates to an effect of the compound represented by the general formula I in inhibiting an NS5B RNA-dependent RNA polymerase (NS5B polymerase for short) which is necessary in a replication process of hepatitis c virus, also relates to an application of the compound, and pharmaceutically acceptable salts, hydrates or prodrugs of the compound in preparation of medicines for treating viral diseases, and especially relates to an application in preparation of medicines for treating and/or preventinghepatitis c.
Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B
Liu, Moyi,Xu, Qiaoling,Guo, Su,Zuo, Ruixi,Hong, Yue,Luo, Yong,Li, Yingxiu,Gong, Ping,Liu, Yajing
, p. 2621 - 2631 (2018/04/30)
The hepatitis C virus (HCV) NS5B polymerase is an attractive target for the development of novel and selective inhibitors of HCV replication. In this paper, the design, synthesis, and preliminary SAR studies of novel inhibitors of HCV NS5B polymerase based on the structure of tegobuvir have been described. The efforts to optimize the antiviral potency and reduce the treatment side effects with respect to genotype 1b resulted in the discovery of compound 3, which exhibited an EC50 of 1.163 nM and a CC50 >200 nM in a cell-based HCV replicon system assay. Additionally, testing for inhibition of the hERG channel showed a marked improvement over tegobuvir and the pharmacokinetic properties of compound 3 indicated that it was worthy of further investigation as a non-nucleoside inhibitor of HCV NS5B polymerase.