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. 2021 May 24;11(31):18748–18756. doi: 10.1039/d1ra00997d

Protease inhibitor activity screening of 3 and 4.

Protease Compound 3a/[%] Compound 4a/[%]
Cathepsin L 7.3 ± 3.3 11 ± 5.0
Cathepsin B 4.9 ± 1.4 n.i.
uPa n.i. n.i.
SrtA 3.8 ± 6.4 2.5 ± 4.2
Rhodesain 5.7 ± 5.2 15 ± 4.6
Cruzain 3.6 ± 2.3 3.8 ± 5.4
Mpro (SARS-CoV2) n.i. 11 ± 9
PLpro (SARS-CoV) n.i. 11 ± 14
DENV2 n.i. 4.8 ± 4.8
ZIKV 0.7 ± 1.2 17 ± 3.4
a

Inhibition at a compound concentration of 200 μM in DMSO as a percentage mean value ± standard deviation with n = 3. Inhibition rates below 0.5% are given as n.i. (no inhibition).