Journal of medicinal chemistry, 09 February 2006, Vol.49(3), pp.1198-201
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.
Antiviral Agents -- Chemical Synthesis ; Dipeptides -- Chemical Synthesis ; Sars Virus -- Drug Effects
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