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Discovery of 8-Hydroxyadenines as a Novel Type of Interferon Inducer

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journal contribution
posted on 09.11.2002, 00:00 by Kosaku Hirota, Kazunori Kazaoka, Itaru Niimoto, Hiroshi Kumihara, Hironao Sajiki, Yoshiaki Isobe, Haruo Takaku, Masanori Tobe, Haruhisa Ogita, Tetsuhiro Ogino, Shinji Ichii, Ayumu Kurimoto, Hajime Kawakami
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 (3032), 2-butylamino (41), and 2-butoxy (47) analogues indicated the highest activities by oral administration to mice.

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