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1.
Acta Pharmaceutica Sinica ; (12): 1378-1387, 2016.
Article in Chinese | WPRIM | ID: wpr-779558

ABSTRACT

Direct acting antivirals against the hepatitis C virus (HCV) have been developed and the field has been under a rapid progress in recent years. Especially, HCV inhibitors targeting nonstructural 5A (NS5A) protein are attracting much attention due to the potent antiviral activity, fast viral clearance and broad antiviral spectrum. This article is prepared to cover the main progress of HCV NS5A complex inhibitors in the market since 2010. The pharmaceutical characteristics of diverse compounds are described and summarized according to their different chemotypes.

2.
Acta Pharmaceutica Sinica ; (12): 947-2016.
Article in Chinese | WPRIM | ID: wpr-779261

ABSTRACT

In order to find more potential DPP-IV inhibitor, a series of xanthine-scaffold analogs of linagliptin, an approved antidiabetes drug, were designed and synthesized for SAR study. All compounds with a concentration of 50 nmol·L-1 showed the inhibitory activity against DPP-IV enzyme in vitro, and the inhibition rate of compounds 1a, 1d and 1f was over 50%. Virtual docking was also performed to facilitate the SAR analysis of these substituted xanthines.

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