Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors.
Identifieur interne : 004128 ( Main/Merge ); précédent : 004127; suivant : 004129Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors.
Auteurs : Han-Zhong Zhang [États-Unis] ; Hong Zhang ; William Kemnitzer ; Ben Tseng ; Jindrich Cinatl ; Martin Michaelis ; Hans Wilhelm Doerr ; Sui Xiong CaiSource :
- Journal of medicinal chemistry [ 0022-2623 ] ; 2006.
Descripteurs français
- KwdFr :
- MESH :
- pharmacologie : Antiviraux, Dipeptides.
- synthèse chimique : Antiviraux, Dipeptides.
- Animaux, Antiviraux, Cellules Caco-2, Cellules Vero, Conception de médicament, Dipeptides, Humains, Mort cellulaire, Réplication virale, Virus du SRAS.
English descriptors
- KwdEn :
- Animals, Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Caco-2 Cells, Cell Death (drug effects), Chlorocebus aethiops, Dipeptides (chemical synthesis), Dipeptides (chemistry), Dipeptides (pharmacology), Drug Design, Humans, SARS Virus (drug effects), Vero Cells, Virus Replication.
- MESH :
- chemical , chemical synthesis : Antiviral Agents, Dipeptides.
- chemical , chemistry : Antiviral Agents, Dipeptides.
- chemical , pharmacology : Antiviral Agents, Dipeptides.
- drug effects : Cell Death, SARS Virus.
- Animals, Caco-2 Cells, Chlorocebus aethiops, Drug Design, Humans, Vero Cells, Virus Replication.
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.
DOI: 10.1021/jm0507678
PubMed: 16451084
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pubmed:16451084Le document en format XML
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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.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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