【摘 要】
：
The high prevalence of hepatitis C virus (HCV) infection and limited treatment options provide an opportunity to develop new therapeutics.The HCV NS3/4A serine protease is an essential enzyme for the
【机 构】
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Anacor Pharmaceuticals,Inc.USA
【出 处】
：
中国上海第七届国际新药发明科技年会
论文部分内容阅读
The high prevalence of hepatitis C virus (HCV) infection and limited treatment options provide an opportunity to develop new therapeutics.The HCV NS3/4A serine protease is an essential enzyme for the replication of the virus and therefore one of the key targets for intervention.We have designed and synthesized a novel series of cyclic boronates and coupled them successfully to several acyclic tripeptide templates at P 1 region.These compounds are inhibitors of the HCV NS3/4A protease,and structural studies show the boronates inhibiting NS3/4A serine protease by trapping Ser-139 hydroxyl group in the enzyme active site.Synthetic methodologies and SAR of this series of compounds will be presented.
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