Structure-based design, synthesis, and evaluation of peptide-mimetic SARS 3CL protease inhibitors

…, Y Hattori, T Ozaki, M Kusunoki, A Sanjoh

Index: Akaji, Kenichi; Konno, Hiroyuki; Mitsui, Hironori; Teruya, Kenta; Shimamoto, Yasuhiro; Hattori, Yasunao; Ozaki, Takeshi; Kusunoki, Masami; Sanjoh, Akira Journal of Medicinal Chemistry, 2011 , vol. 54, # 23 p. 7962 - 7973

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Citation Number: 25

Abstract

The design and evaluation of low molecular weight peptide-based severe acute respiratory syndrome (SARS) chymotrypsin-like protease (3CL) protease inhibitors are described. A substrate-based peptide aldehyde was selected as a starting compound, and optimum side- chain structures were determined, based on a comparison of inhibitory activities with Michael type inhibitors. For the efficient screening of peptide aldehydes containing a ...