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

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

Bioorganic & medicinal chemistry letters (2007-03-06)
Masahiro Ikejiri, Masayuki Saijo, Shigeru Morikawa, Shuetsu Fukushi, Tetsuya Mizutani, Ichiro Kurane, Tokumi Maruyama
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
6-Chloropurine, ≥99%
Sigma-Aldrich
6-Chloropurine, 99%
Sigma-Aldrich
6-Chloropurine riboside, 99%