1. Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of
- Author
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Guangyi, Wang, Natalia, Dyatkina, Marija, Prhavc, Caroline, Williams, Vladimir, Serebryany, Yujian, Hu, Yongfei, Huang, Xiangyang, Wu, Tongqian, Chen, Wensheng, Huang, Vivek K, Rajwanshi, Jerome, Deval, Amy, Fung, Zhinan, Jin, Antitsa, Stoycheva, Kenneth, Shaw, Kusum, Gupta, Yuen, Tam, Andreas, Jekle, David B, Smith, and Leonid, Beigelman
- Subjects
Male ,Dogs ,Animals ,Humans ,Female ,Prodrugs ,DNA-Directed RNA Polymerases ,Hepacivirus ,Enzyme Inhibitors ,Viral Nonstructural Proteins ,Virus Replication ,Antiviral Agents ,Guanine Nucleotides - Abstract
Chronic hepatitis C (CHC) is a major liver disease caused by the hepatitis C virus. The current standard of care for CHC can achieve cure rates above 95%; however, the drugs in current use are administered for a period of 8-16 weeks. A combination of safe and effective drugs with a shorter treatment period is highly desirable. We report synthesis and biological evaluation of a series of 2',3'- and 2',4'-substituted guanosine nucleotide analogues. Their triphosphates exhibited potent inhibition of the HCV NS5B polymerase with IC
- Published
- 2020