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Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors.

Authors
  • Ghosh, Arun K
  • Xi, Kai
  • Ratia, Kiira
  • Santarsiero, Bernard D
  • Fu, Wentao
  • Harcourt, Brian H
  • Rota, Paul A
  • Baker, Susan C
  • Johnson, Michael E
  • Mesecar, Andrew D
Type
Published Article
Journal
Journal of medicinal chemistry
Publication Date
Nov 03, 2005
Volume
48
Issue
22
Pages
6767–6771
Identifiers
PMID: 16250632
Source
Medline
License
Unknown

Abstract

Design, synthesis, and biological evaluation of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease (SARS-3CLpro) inhibitors for severe acute respiratory syndrome coronavirus (SARS-CoV) are described. These inhibitors exhibited antiviral activity against SARS-CoV in infected cells in the micromolar range. An X-ray crystal structure of our lead inhibitor (4) bound to SARS-3CLpro provided important drug-design templates for the design of small-molecule inhibitors.

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