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Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents

Identifieur interne : 003B21 ( Main/Exploration ); précédent : 003B20; suivant : 003B22

Synthesis 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 :

RBID : Pascal:07-0465126

Descripteurs français

English descriptors

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.


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Le document en format XML

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<term>Chemical synthesis</term>
<term>Chemistry, Pharmaceutical (methods)</term>
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<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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