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
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DOI：
10.1016/j.bmcl.2007.02.026
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发表时间：
2007-05-01
影响因子：
2.7
通讯作者：
Maruyama, Tokumi
中科院分区：
文献类型：
--
作者：
Ikejiri, Masahiro;Saijo, Masayuki;Maruyama, Tokumi
为了开发新型抗SARS冠状病毒药物，合成了以6-氯嘌呤为碱基的核苷类似物，并通过空斑减少和产率降低实验评价了其抗SARS-CoV活性。在这些类似物中，有两个化合物，即I和11，具有与已知的抗SARS-CoV药物咪唑立宾和利巴韦林相媲美的抗SARS-CoV活性。此外，我们还观察了6-氯嘌呤部分、未保护的5‘-羟基和苯甲酰化5’-羟基的抗病毒作用等几个SAR趋势。(C)2007爱思唯尔有限公司。保留所有权利。
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.