Issue 10, 2013

Synthesis, activity and structure–activity relationship of noroviral protease inhibitors

Abstract

The protease of norovirus, an important human pathogen, is essential for the viral replication and, therefore, represents a potential drug target. A series of tripeptide-based inhibitors of the protease were designed, synthesized and tested, among which several potent inhibitors were identified with Ki values as low as 75 nM. The structure–activity relationships of these inhibitors are discussed.

Graphical abstract: Synthesis, activity and structure–activity relationship of noroviral protease inhibitors

Supplementary files

Article information

Article type
Concise Article
Submitted
29 Jul 2013
Accepted
02 Sep 2013
First published
03 Sep 2013

Med. Chem. Commun., 2013,4, 1354-1359

Synthesis, activity and structure–activity relationship of noroviral protease inhibitors

L. Deng, Z. Muhaxhiri, M. K. Estes, T. Palzkill, B. V. Venkataram Prasad and Y. Song, Med. Chem. Commun., 2013, 4, 1354 DOI: 10.1039/C3MD00219E

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