Discovery of 8-hydroxyadenines as a novel type of interferon inducer

被引:75
|
作者
Hirota, K [1 ]
Kazaoka, K
Niimoto, I
Kumihara, H
Sajiki, H
Isobe, Y
Takaku, H
Tobe, M
Ogita, H
Ogino, T
Ichii, S
Kurimoto, A
Kawakami, H
机构
[1] Gifu Pharmaceut Univ, Med Chem Lab, Gifu 5028585, Japan
[2] Japan Energy Corp, Pharmaceut & Biotechnol Lab, Toda, Saitama 3350026, Japan
[3] Sumitomo Pharmaceut, Div Res, Konohana Ku, Osaka 5540022, Japan
关键词
D O I
10.1021/jm0203581
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
9-Benzyl-8-hydroxyadenine (6) was found to possess interferon-inducing activity in vitro as a lead compound. Although replacement of the 9-benzyl group of 6 did not improve the activity, the introduction of a substituent such as alkyl, alkylthio, alkylamino, and alkoxy groups into the 2-position of the adenine ring resulted in a remarkable increase in the activity. The 2-alkylthio (30-32), 2-butylamino (41), and 2-butoxy (47) analogues indicated the highest activities by oral administration to mice.
引用
收藏
页码:5419 / 5422
页数:4
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