Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Lu Zhou; Ying Liu; Weilin Zhang; Ping Wei; Changkang Huang; Jianfeng Pei; Yaxia Yuan; Luhua Lai

doi:10.1021/jm0602357

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Lu Zhou, Ying Liu, Weilin Zhang, Ping Wei, Changkang Huang, Jianfeng Pei, Yaxia Yuan, Luhua Lai

Research output: Contribution to journal › Article › peer-review

127 Scopus citations

Abstract

A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound Sf shows significant inhibition with an IC₅₀ of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.

Original language	English (US)
Pages (from-to)	3440-3443
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	49
Issue number	12
DOIs	https://doi.org/10.1021/jm0602357
State	Published - Jun 15 2006
Externally published	Yes

ASJC Scopus subject areas

Drug Discovery
Molecular Medicine

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title = "Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors",

abstract = "A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound Sf shows significant inhibition with an IC50 of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.",

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AU - Zhou, Lu

AU - Liu, Ying

AU - Zhang, Weilin

AU - Wei, Ping

AU - Huang, Changkang

AU - Pei, Jianfeng

AU - Yuan, Yaxia

AU - Lai, Luhua

PY - 2006/6/15

Y1 - 2006/6/15

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AB - A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound Sf shows significant inhibition with an IC50 of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.

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IS - 12

ER -

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Abstract

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