Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease.

Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease.
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DOI:
10.1016/j.bmcl.2011.07.016
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发表时间:
2011-09-15
影响因子:
2.7
通讯作者:
Groutas, William C.
Groutas, William C.
中科院分区:
医学4区
文献类型:
--
作者:
Tiew, Kok-Chuan;He, Guijia;Aravapalli, Sridhar;Mandadapu, Sivakoteswara Rao;Gunnam, Mallikarjuna Reddy;Alliston, Kevin R.;Lushington, Gerald H.;Kim, Yunjeong;Chang, Kyeong-Ok;Groutas, William C.

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The first series of peptidyl aldehyde inhibitors that incorporate in their structure a glutamine surrogate has been designed and synthesized based on the known substrate specificity of Norwalk virus 3C protease. The inhibitory activity of the compounds with the protease and with a norovirus cell-based replicon system was investigated. Members of this class of compounds exhibited noteworthy activity both in vitro and in a cell-based replicon system.
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