The application of phosphoramidate ProTide technology to the potent anti-HCV compound 4'-azidocytidine (R1479).
Identifieur interne : 002997 ( Main/Exploration ); précédent : 002996; suivant : 002998The application of phosphoramidate ProTide technology to the potent anti-HCV compound 4'-azidocytidine (R1479).
Auteurs : Christopher Mcguigan [Royaume-Uni] ; Mary Rose Kelleher ; Plinio Perrone ; Sinead Mulready ; Giovanna Luoni ; Felice Daverio ; Sonal Rajyaguru ; Sophie Le Pogam ; Isabel Najera ; Joseph A. Martin ; Klaus Klumpp ; David B. SmithSource :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2009.
Descripteurs français
- KwdFr :
- Acides aminés (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Chimie pharmaceutique (), Conception de médicament, Cytidine (analogues et dérivés), Cytidine (pharmacologie), Cytidine (synthèse chimique), Hepacivirus (métabolisme), Humains, Hépatite C (traitement médicamenteux), Modèles chimiques, Promédicaments, Réplication virale, Réplicon (), Technologie pharmaceutique (), Évaluation préclinique de médicament.
- MESH :
- analogues et dérivés : Cytidine.
- métabolisme : Hepacivirus.
- pharmacologie : Antiviraux, Cytidine.
- synthèse chimique : Antiviraux, Cytidine.
- traitement médicamenteux : Hépatite C.
- Acides aminés, Chimie pharmaceutique, Conception de médicament, Humains, Modèles chimiques, Promédicaments, Réplication virale, Réplicon, Technologie pharmaceutique, Évaluation préclinique de médicament.
English descriptors
- KwdEn :
- Amino Acids (chemistry), Antiviral Agents (chemical synthesis), Antiviral Agents (pharmacology), Chemistry, Pharmaceutical (methods), Cytidine (analogs & derivatives), Cytidine (chemical synthesis), Cytidine (pharmacology), Drug Design, Drug Evaluation, Preclinical, Hepacivirus (metabolism), Hepatitis C (drug therapy), Humans, Models, Chemical, Prodrugs, Replicon (drug effects), Technology, Pharmaceutical (methods), Virus Replication.
- MESH :
- chemical , analogs & derivatives : Cytidine.
- chemical , chemical synthesis : Antiviral Agents, Cytidine.
- chemical , chemistry : Amino Acids.
- chemical , pharmacology : Antiviral Agents, Cytidine.
- drug effects : Replicon.
- drug therapy : Hepatitis C.
- metabolism : Hepacivirus.
- methods : Chemistry, Pharmaceutical, Technology, Pharmaceutical.
- Drug Design, Drug Evaluation, Preclinical, Humans, Models, Chemical, Prodrugs, Virus Replication.
Abstract
We report the design, synthesis and evaluation of a family of ca 50 phosphoramidate ProTides of the potent anti-HCV compound 4'-azidocytidine (R1479), with variation on the ester, amino acid and aryl moiety of the ProTide. Sub-muM inhibitors of HCV emerge. The compounds are all non-cytotoxic in the replicon assay. We herein report detailed SARs for each of the regions of the ProTide.
DOI: 10.1016/j.bmcl.2009.05.099
PubMed: 19505826
Affiliations:
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Sub-muM inhibitors of HCV emerge. The compounds are all non-cytotoxic in the replicon assay. We herein report detailed SARs for each of the regions of the ProTide.</div></front></TEI><affiliations><list><country><li>Royaume-Uni</li></country></list><tree><noCountry><name sortKey="Daverio, Felice" sort="Daverio, Felice" uniqKey="Daverio F" first="Felice" last="Daverio">Felice Daverio</name><name sortKey="Kelleher, Mary Rose" sort="Kelleher, Mary Rose" uniqKey="Kelleher M" first="Mary Rose" last="Kelleher">Mary Rose Kelleher</name><name sortKey="Klumpp, Klaus" sort="Klumpp, Klaus" uniqKey="Klumpp K" first="Klaus" last="Klumpp">Klaus Klumpp</name><name sortKey="Le Pogam, Sophie" sort="Le Pogam, Sophie" uniqKey="Le Pogam S" first="Sophie" last="Le Pogam">Sophie Le Pogam</name><name sortKey="Luoni, Giovanna" sort="Luoni, Giovanna" uniqKey="Luoni G" first="Giovanna" last="Luoni">Giovanna Luoni</name><name sortKey="Martin, Joseph A" sort="Martin, Joseph A" uniqKey="Martin J" first="Joseph A" last="Martin">Joseph A. Martin</name><name sortKey="Mulready, Sinead" sort="Mulready, Sinead" uniqKey="Mulready S" first="Sinead" last="Mulready">Sinead Mulready</name><name sortKey="Najera, Isabel" sort="Najera, Isabel" uniqKey="Najera I" first="Isabel" last="Najera">Isabel Najera</name><name sortKey="Perrone, Plinio" sort="Perrone, Plinio" uniqKey="Perrone P" first="Plinio" last="Perrone">Plinio Perrone</name><name sortKey="Rajyaguru, Sonal" sort="Rajyaguru, Sonal" uniqKey="Rajyaguru S" first="Sonal" last="Rajyaguru">Sonal Rajyaguru</name><name sortKey="Smith, David B" sort="Smith, David B" uniqKey="Smith D" first="David B" last="Smith">David B. Smith</name></noCountry><country name="Royaume-Uni"><noRegion><name sortKey="Mcguigan, Christopher" sort="Mcguigan, Christopher" uniqKey="Mcguigan C" first="Christopher" last="Mcguigan">Christopher Mcguigan</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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