Key result
Isatin derivative Compound 5f reversibly inhibits SARS-CoV 3C-like protease at ~0.37 microM.
Why the study?
Differences in substrate binding sites between rhinovirus 3C protease and SARS CoV 3C-like protease were unclear, motivating testing of isatin derivatives as inhibitors.
Answers are grounded in this paper and cite their sources.
Isatin derivatives, particularly Compound 5f, act as noncovalent reversible inhibitors of the SARS CoV 3C-like protease.
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 IC(50) of 0.37 microM. 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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Zhou et al. (2006) studied SARS CoV 3C-like protease. Isatin derivatives (Compound 5f) was evaluated on Inhibition of SARS CoV 3C-like protease (IC50 0.37 microM). Isatin derivative Compound 5f demonstrated significant noncovalent, reversible inhibition of SARS CoV 3C-like protease with an IC50 of 0.37 microM.
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