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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.

SUBMITTER: Deng L

PROVIDER: S-EPMC3826262 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature

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Synthesis, Activity and Structure-Activity Relationship of Noroviral Protease Inhibitors.

Deng Lisheng L Muhaxhiri Zana Z Estes Mary K MK Palzkill Timothy T Prasad B V Venkataram BV Song Yongcheng Y

MedChemComm 20131001 10

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 K<sub>i</sub> values as low as 75 nM. The structure-activity relationships of these inhibitors are discussed. ...[more]

PMID: 24244836

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