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Bioorg Med Chem Lett. 2013 Aug 15;23(16):4528-31. doi: 10.1016/j.bmcl.2013.06.045. Epub 2013 Jun 26.

Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents.

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  • 1Key Laboratory of Medical Molecular Virology, Shanghai Medical College, Fudan University, 138 Yi-Xue-Yuan Road, Shanghai 200032, PR China.


A series of diketo tetrazoles and diketo triazoles were designed and synthesized as bioisosteres of α,γ-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 μM 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 α,γ-diketo acid to exhibit potent inhibitory activity against HCV.

Copyright © 2013 Elsevier Ltd. All rights reserved.


Anti-HCV activity; Bioisosteres; Diketo tetrazoles; Diketo triazoles

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