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_38
Snippet: In addition to better matching the H-bonding donor/acceptor properties of the catalytic center through offering two hydrogen-bond acceptors instead of one, a-ketoamides have another big advantage over aldehydes and a,b-unsaturated esters (Michael acceptors) in that they allow easy extension of the inhibitors to probe the primed specificity subsites beyond S1', although this has so far rarely been explored (e.g., ref. 38 in case of calpain)......
Document: In addition to better matching the H-bonding donor/acceptor properties of the catalytic center through offering two hydrogen-bond acceptors instead of one, a-ketoamides have another big advantage over aldehydes and a,b-unsaturated esters (Michael acceptors) in that they allow easy extension of the inhibitors to probe the primed specificity subsites beyond S1', although this has so far rarely been explored (e.g., ref. 38 in case of calpain).
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