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

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

  • J Med Chem. 2006 Feb 9;49(3):1198-201. doi: 10.1021/jm0507678.
Han-Zhong Zhang 1,  Hong Zhang,  William Kemnitzer,  Ben Tseng,  Jindrich Cinatl Jr,  Martin Michaelis,  Hans Wilhelm Doerr,  Sui Xiong Cai
Affiliations

Affiliation

  • 1 Maxim Pharmaceuticals, 6650 Nancy Ridge Drive, San Diego, CA 92121, USA.
PMID: 16451084 DOI: 10.1021/jm0507678
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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