Author: Linlin Zhang; Daizong Lin; Yuri Kusov; Yong Nian; Qingjun Ma; Jiang Wang; Albrecht von Brunn; Pieter Leyssen; Kristina Lanko; Johan Neyts; Adriaan de Wilde; Eric J. Snijder; Hong Liu; Rolf Hilgenfeld
Title: Alpha-ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication Document date: 2020_2_10
ID: 7n8p9okf_43
Snippet: For compounds with warheads other than a-ketoamides, in-vitro activity against both corona-and enteroviruses has also occasionally been reported. Lee et al. 46 described three peptidyl Michael acceptors that displayed inhibitory activity against the M pro s of SARS-CoV and HCoV 229E as well as against the 3C pro of CVB3. These inhibitors had an IC50 10 -20 times higher for the CVB3 enzyme, compared to SARS-CoV M pro . P2 was invariably isobutyl (.....
Document: For compounds with warheads other than a-ketoamides, in-vitro activity against both corona-and enteroviruses has also occasionally been reported. Lee et al. 46 described three peptidyl Michael acceptors that displayed inhibitory activity against the M pro s of SARS-CoV and HCoV 229E as well as against the 3C pro of CVB3. These inhibitors had an IC50 10 -20 times higher for the CVB3 enzyme, compared to SARS-CoV M pro . P2 was invariably isobutyl (leucine) in these compounds, suggesting that further improvement might be possible.
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