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_27
Snippet: When we replaced the P2-isobutyl residue of 11n by n-butyl in 11o, the activities were as follows: IC50 = 8.5 µM for SARS-CoV M pro , totally inactive (IC50 > 50 µM) against HCoV-NL63 M pro , IC50 = 3.2 µM for EV-A71 3C pro , and 5.2 µM for CVB3 3C pro . The decreased activity in case of SARS-CoV M pro and the total inactivity against HCoV-NL63 M pro indicate that the n-butyl chain is too long for the S2 pocket of these proteases, whereas the.....
Document: When we replaced the P2-isobutyl residue of 11n by n-butyl in 11o, the activities were as follows: IC50 = 8.5 µM for SARS-CoV M pro , totally inactive (IC50 > 50 µM) against HCoV-NL63 M pro , IC50 = 3.2 µM for EV-A71 3C pro , and 5.2 µM for CVB3 3C pro . The decreased activity in case of SARS-CoV M pro and the total inactivity against HCoV-NL63 M pro indicate that the n-butyl chain is too long for the S2 pocket of these proteases, whereas the slight improvement against EV-A71 3C pro and CVB3 3C pro is probably a consequence of the extra space that is available to long and flexible substituents because of the lack of a lid covering the enterovirus 3C pro pocket.
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