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. 2006 Feb 9;49(3):1198-201.
doi: 10.1021/jm0507678.

Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors

Han-Zhong Zhang  1 , Hong Zhang, William Kemnitzer, Ben Tseng, Jindrich Cinatl Jr, Martin Michaelis, Hans Wilhelm Doerr, Sui Xiong Cai
Affiliations

Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors

Han-Zhong Zhang et al. J Med Chem. .

Abstract

This paper describes the design and synthesis of dipeptidyl N,N-dimethyl glutaminyl fluoromethyl ketones (fmk) as severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors. The compounds were tested against SARS-CoV-induced cell death in Vero or CaCo2 cells as a measurement of the inhibiting effects of the compounds on the replication of the virus. Z-Leu-Gln(NMe(2))-fmk (6a) was found to be a potent inhibitor with low toxicity in cells, protecting cells with an EC(50) value of 2.5 microM and exhibiting a selectivity index of >40.

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