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Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.


ABSTRACT: 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? showed most potent inhibitory activity against 3CL(pro) (IC??=1.04 ?M). These results indicated that these inhibitors could be potentially developed into anti-SARS drugs.

SUBMITTER: Liu W 

PROVIDER: S-EPMC7111328 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.

Liu Wei W   Zhu He-Min HM   Niu Guo-Jun GJ   Shi En-Zhi EZ   Chen Jie J   Sun Bo B   Chen Wei-Qiang WQ   Zhou Hong-Gang HG   Yang Cheng C  

Bioorganic & medicinal chemistry 20131121 1


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 vitr  ...[more]

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