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Bioorg Med Chem Lett. 2009 Jan 1;19(1):180-3. doi: 10.1016/j.bmcl.2008.10.124. Epub 2008 Nov 5.

Potent inhibitors of HCV-NS3 protease derived from boronic acids.

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  • 1Schering Plough Research Institute, K15-MS 3545, Kenilworth, NJ 07033, USA.


Chronic hepatitis C infection is the leading causes for cirrhosis of the liver and hepatocellular carcinoma, leading to liver failure and liver transplantation. The etiological agent, HCV virus produces a single positive strand of RNA that is processed with the help of serine protease NS3 to produce mature virus. Inhibition of NS3 protease can be potentially used to develop effective drugs for HCV infections. Numerous efforts are now underway to develop potent inhibitors of HCV protease that contain ketoamides as serine traps. Herein we report the synthesis of a series of potent inhibitors that contain a boronic acid as a serine trap. The activity of these compounds were optimized to 200pM. X-ray structure of compound 17 bound to NS3 protease is also discussed.

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