Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents
Identifieur interne : 003B21 ( Main/Exploration ); précédent : 003B20; suivant : 003B22Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents
Auteurs : Masahiro Ikejiri [Japon] ; Masayuki Saijo [Japon] ; Shigeru Morikawa [Japon] ; Shuetsu Fukushi [Japon] ; Tetsuya Mizutani [Japon] ; Ichiro Kurane [Japon] ; Tokumi Maruyama [Japon]Source :
- Bioorganic & medicinal chemistry letters : (Print) [ 0960-894X ] ; 2007.
Descripteurs français
- KwdFr :
- Animaux, Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cellules Vero, Chimie pharmaceutique (), Concentration inhibitrice 50, Conception de médicament, Conformation moléculaire, Modèles chimiques, Nucléosides (pharmacologie), Nucléosides (synthèse chimique), Purines (), Relation dose-effet des médicaments, Syndrome respiratoire aigu sévère (traitement médicamenteux), Virus du SRAS (métabolisme), Études d'évaluation comme sujet.
- MESH :
- métabolisme : Virus du SRAS.
- pharmacologie : Antiviraux, Nucléosides.
- synthèse chimique : Antiviraux, Nucléosides.
- traitement médicamenteux : Syndrome respiratoire aigu sévère.
- Pascal (Inist)
- Animaux, Cellules Vero, Chimie pharmaceutique, Concentration inhibitrice 50, Conception de médicament, Conformation moléculaire, Modèles chimiques, Purines, Relation dose-effet des médicaments, Synthèse chimique, Relation structure activité, Analogue nucléoside, Antiviral, Virus syndrome respiratoire aigu sévère, Purine nucléoside, In vitro, Purine(9-[3-benzoyloxy-2-(hydroxyméthyl)cyclobutyl]-6-chloro), Cyclobutane-1,2-diméthanol dérivé, 1,2,4-Triazole dérivé, Études d'évaluation comme sujet.
English descriptors
- KwdEn :
- Animals, Antiviral, Antiviral Agents (chemical synthesis), Antiviral Agents (pharmacology), Chemical synthesis, Chemistry, Pharmaceutical (methods), Chlorocebus aethiops, Dose-Response Relationship, Drug, Drug Design, Evaluation Studies as Topic, In vitro, Inhibitory Concentration 50, Models, Chemical, Molecular Conformation, Nucleoside analog, Nucleosides (chemical synthesis), Nucleosides (pharmacology), Purine nucleoside, Purines (chemistry), SARS Virus (metabolism), Severe Acute Respiratory Syndrome (drug therapy), Severe acute respiratory syndrome virus, Structure activity relation, Vero Cells.
- MESH :
- chemical , chemical synthesis : Antiviral Agents, Nucleosides.
- chemical , chemistry : Purines.
- chemical , pharmacology : Antiviral Agents, Nucleosides.
- drug therapy : Severe Acute Respiratory Syndrome.
- metabolism : SARS Virus.
- methods : Chemistry, Pharmaceutical.
- Animals, Chlorocebus aethiops, Dose-Response Relationship, Drug, Drug Design, Evaluation Studies as Topic, Inhibitory Concentration 50, Models, Chemical, Molecular Conformation, Vero Cells.
Abstract
Nucleoside analogues that have 6-chloropurine as the nucleobase were synthesized and evaluated for anti-SARS-CoV activity by plaque reduction and yield reduction assays in order to develop novel anti-SARS-CoV agents. Among these analogues, two compounds, namely, 1 and 11, exhibited promising anti-SARS-CoV activity that was comparable to those of mizoribine and ribavirin, which are known anti-SARS-CoV agents. Moreover, we observed several SAR trends such as the antiviral effects of the 6-chloropurine moiety, unprotected 5'-hydroxyl group and benzoylated 5'-hydroxyl group.
Affiliations:
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Le document en format XML
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<term>Chemical synthesis</term>
<term>Chemistry, Pharmaceutical (methods)</term>
<term>Chlorocebus aethiops</term>
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<term>Drug Design</term>
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<term>Nucleosides (pharmacology)</term>
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<term>Severe Acute Respiratory Syndrome (drug therapy)</term>
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<term>Structure activity relation</term>
<term>Vero Cells</term>
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<term>Conception de médicament</term>
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<term>Nucléosides (synthèse chimique)</term>
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<term>Virus du SRAS (métabolisme)</term>
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<front><div type="abstract" xml:lang="en">Nucleoside analogues that have 6-chloropurine as the nucleobase were synthesized and evaluated for anti-SARS-CoV activity by plaque reduction and yield reduction assays in order to develop novel anti-SARS-CoV agents. Among these analogues, two compounds, namely, 1 and 11, exhibited promising anti-SARS-CoV activity that was comparable to those of mizoribine and ribavirin, which are known anti-SARS-CoV agents. Moreover, we observed several SAR trends such as the antiviral effects of the 6-chloropurine moiety, unprotected 5'-hydroxyl group and benzoylated 5'-hydroxyl group.</div>
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