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_28
Snippet: As the n-butyl substituent in P2 of 11o was obviously too long, we next synthesized a derivative with the shorter propargyl (ethinylmethyl) as the P2 residue (compound 11p). This led to very mediocre activities against all tested proteases. Using cyclopropyl as the P2 residue (compound 11q), the IC50 values were even higher against most of the proteases tested. Obviously, the P2 side-chain requires a methylene group in the b-position in order to .....
Document: As the n-butyl substituent in P2 of 11o was obviously too long, we next synthesized a derivative with the shorter propargyl (ethinylmethyl) as the P2 residue (compound 11p). This led to very mediocre activities against all tested proteases. Using cyclopropyl as the P2 residue (compound 11q), the IC50 values were even higher against most of the proteases tested. Obviously, the P2 side-chain requires a methylene group in the b-position in order to provide the necessary flexibility for the substituent to be embedded in the S2 pocket.
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