Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 16, Pages 4528-4531Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.045
Keywords
Anti-HCV activity; Diketo tetrazoles; Diketo triazoles; Bioisosteres
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Funding
- National Natural Science Foundation of China [20902013, 30973641]
- National Basic Research Program of China [2009CB522504]
- Shanghai Committee of Science and Technology of China [13ZR1403900]
- China Postdoctoral Science Foundation [2013M531126]
- Zhuo Xue Program of Fudan University
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A series of diketo tetrazoles and diketo triazoles were designed and synthesized as bioisosteres of alpha,gamma-diketo acid, the active site inhibitor of HCV (Hepatitis C virus) polymerase NS5B. Among the synthesized compounds, 4-(4-fluorobenzyloxy)phenyl diketo triazole (30) exhibited anti-HCV activity with an EC50 value of 3.9 mu M and an SI value more than 128. The reduction of viral protein and mRNA levels were also validated, supporting the anti-HCV activity of compound 30. These results provide convincing evidence that the diketo tetrazoles and diketo triazoles can be developed as bioisosteres of alpha,gamma-diketo acid to exhibit potent inhibitory activity against HCV. (c) 2013 Elsevier Ltd. All rights reserved.
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