The application of phosphoramidate ProTide technology to the potent anti-HCV compound 4'-azidocytidine (R1479).
Identifieur interne : 001F37 ( Ncbi/Curation ); précédent : 001F36; suivant : 001F38The 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
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pubmed:19505826Le document en format XML
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<front><div type="abstract" xml:lang="en">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.</div>
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