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

ABSTRACT: 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.

SUBMITTER: Tiew KC 

PROVIDER: S-EPMC3159713 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature

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

Tiew Kok-Chuan KC   He Guijia G   Aravapalli Sridhar S   Mandadapu Sivakoteswara Rao SR   Gunnam Mallikarjuna Reddy MR   Alliston Kevin R KR   Lushington Gerald H GH   Kim Yunjeong Y   Chang Kyeong-Ok KO   Groutas William C WC  

Bioorganic & medicinal chemistry letters 20110714 18

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. ...[more]

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