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_30
Snippet: Having realized that in addition to size, flexibility of the P2 substituent may be an important factor influencing inhibitory activity, we introduced flexibility into the phenyl ring of 11a by reducing it. The cyclohexylmethyl derivative 11r exhibited IC50 = 0.7 µM against SARS-CoV M pro , 12.3 µM against HCoV-NL63 M pro , 1.7 µM against EV-A71 3C pro , and 0.9 µM against CVB3 3C pro . Thus, the replace- 1 2 3 4 5 6 7 8 9 10 11 12 .....
Document: Having realized that in addition to size, flexibility of the P2 substituent may be an important factor influencing inhibitory activity, we introduced flexibility into the phenyl ring of 11a by reducing it. The cyclohexylmethyl derivative 11r exhibited IC50 = 0.7 µM against SARS-CoV M pro , 12.3 µM against HCoV-NL63 M pro , 1.7 µM against EV-A71 3C pro , and 0.9 µM against CVB3 3C pro . Thus, the replace- 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 author/funder. All rights reserved. No reuse allowed without permission.
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