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

L Zhou, Y Liu, W Zhang, P Wei, C Huang…

Index: Zhou, Lu; Liu, Ying; Zhang, Weilin; Wei, Ping; Huang, Changkang; Pei, Jianfeng; Yuan, Yaxia; Lai, Luhua Journal of Medicinal Chemistry, 2006 , vol. 49, # 12 p. 3440 - 3443

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Citation Number: 62

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 5f shows significant inhibition with an IC50 of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human ...