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Updated: Aug 30, 2026

Engineering Antiviral Agents via Surface Plasmon Resonance
Published on: June 14, 2022
Synthesis and structure-activity relationships of 2-amino-8-hydroxyadenines as orally active interferon inducing
Ayumu Kurimoto1, Tetsuhiro Ogino, Shinji Ichii
1Research Division, Discovery Research Laboratories II, Sumitomo Pharmaceuticals Co Ltd, Konohana-ku, Osaka 554-0022, Japan. akurimoto@sumitomopharm.co.jp
Abstract:
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%).
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