Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 22, Pages 6767-6771Publisher
AMER CHEMICAL SOC
DOI: 10.1021/JM050548m
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Funding
- NIAID NIH HHS [P01 AI060915, P01 AI 060915, P01 AI060915-030003] Funding Source: Medline
- NIGMS NIH HHS [GM 53386] Funding Source: Medline
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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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