Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 1, Pages 292-302Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.11.028
Keywords
SARS; Inhibitor; Isatin; Docking studies
Funding
- Tianjin SME Technology Innovation Fund [11ZXCXSY03500]
- National Biomedical Special Project of International Innovation Park [11ZCKFSY06800]
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The Severe Acute Respiratory Syndrome (SARS) is a serious life-threatening and strikingly mortal respiratory illness caused by SARS-CoV. SARS-CoV which contains a chymotrypsin-like main protease analogous to that of the main picornavirus protease, 3CL(pro). 3CL(pro) plays a pivotal role in the viral replication cycle and is a potential target for SARS inhibitor development. A series of isatin derivatives as possible SARS-CoV 3CL(pro) inhibitors was designed, synthesized, and evaluated by in vitro protease assay using fluorogenic substrate peptide, in which several showed potent inhibition against the 3CL(pro). Structure-activity relationship was analyzed, and possible binding interaction modes were proposed by molecular docking studies. Among all compounds, 8k(1) showed most potent inhibitory activity against 3CL(pro) (IC50 = 1.04 mu M). These results indicated that these inhibitors could be potentially developed into anti-SARS drugs. (C) 2013 Elsevier Ltd. All rights reserved.
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