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

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^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(18): 5315-5319.

DOI：10.1016/j.bmcl.2011.07.016

• Inhibitors
• Peptidyl aldehydes
• Norwalk virus
• 3C protease
• Transition state inhibitors

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.

• 出版日期2011-9-15