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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:17

Article

Ikejiri, Masahiro ; Saijo, Masayuki ; Morikawa, Shigeru ; Fukushi, Shuetsu ; Mizutani, Tetsuya ; Kurane, Ichiro ; Maruyama, Tokumi

关键词: SARS-CoV;    nucleoside;    6-chloropurine;    antiviral;   

DOI  :  10.1016/j.bmcl.2007.02.026

来源: Elsevier

【 摘 要 】

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, I and 1 1, 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. (C) 2007 Elsevier Ltd. All rights reserved.

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