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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Tiew, Kok-Chuan¹  He, Guijia¹  Aravapalli, Sridhar¹  Mandadapu, Sivakoteswara Rao¹  Gunnam, Mallikarjuna Reddy¹  Alliston, Kevin R.¹  Lushington, Gerald H.²  Kim, Yunjeong³  Chang, Kyeong-Ok³  Groutas, William C.¹ 

[1] Wichita State Univ, Dept Chem, Wichita, KS 67260 USA

[2] Univ Kansas, Mol Graph & Modeling Lab, Lawrence, KS 66045 USA

[3] Kansas State Univ, Coll Vet Med, Dept Diagnost Med Pathobiol, Manhattan, KS 66506 USA

关键词: Inhibitors;    Peptidyl aldehydes;    Norwalk virus;    3C protease;    Transition state inhibitors;   

DOI  :  10.1016/j.bmcl.2011.07.016

来源: Elsevier

【 摘 要 】

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. (C) 2011 Elsevier Ltd. All rights reserved.

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