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

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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Elsevier, Bioorganic and Medicinal Chemistry Letters, 18(21), p. 5315-5319

DOI: 10.1016/j.bmcl.2011.07.016

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

Journal article published in 2011 by Kok-Chuan Tiew, Guijia He, Sridhar Aravapalli, Sivakoteswara Rao Mandadapu, Mallikarjuna Reddy Gunnam, Kevin R. Alliston, Gerald H. Lushington, Yunjeong Kim

, Kyeong-Ok Chang, William C. Groutas

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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.

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

Abstract