226907-95-5Relevant articles and documents
Synthesis and structure-activity relationships of 2-amino-8- hydroxyadenines as orally active interferon inducing agents
Kurimoto, Ayumu,Ogino, Tetsuhiro,Ichii, Shinji,Isobe, Yoshiaki,Tobe, Masanori,Ogita, Haruhisa,Takaku, Haruo,Sajiki, Hironao,Hirota, Kosaku,Kawakami, Hajime
, p. 5501 - 5508 (2003)
Recently, we have reported the 8-hydroxyadenine derivatives (2-4) as a novel class of interferon (IFN) inducing agents. In the present study, a series of 8-hydroxyadenines, which possess various amino moieties at the adenine C(2)-position, were synthesized and evaluated for their ability to induce endogenous IFN in comparison to the known active agent, Imiquimod. Among the compounds prepared, compound 9o possessing a 2-methoxyethylamino group at C(2)-position of adenine was found to exhibit potent IFN inducing activity in vivo. Compound 9o induced IFN from the dosage of 0.1 mg/kg, which was 30-fold potent than that of Imiquimod, and showed a good oral bioavailability (F=81%).