Bioorganic & Medicinal Chemistry Letters 2007-05-01

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

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

Index: Bioorg. Med. Chem. Lett. 17 , 2470-3, (2007)

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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.