Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 12, Issue 5, Pages 1091-1099Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2003.12.008
Keywords
8-hydroxyadenines; orally active; interferon inducer; HCV; imiquimod
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In order to create novel compounds which possess potent interferon (IFN) inducing activities with excellent oral bioavailabilities, a series of 8-hydroxyadenines, which have various alkoxy or alkylthio moieties at the adenine C(2)-position, were synthesized and evaluated. The introduction of hydrophobic groups was not considered to be effective for potentiating the IFN-inducing activity, but several compounds having hydrophilic groups were effective. Among the compounds tested, compound 13f induced IFN from the dosage of 0.03 mg/kg, which was approximately 100-fold more potent than that of Imiquimod, and showed an excellent oral bioavailability (F = 40%) which was 10-fold improved over 5, a lead compound (F = 4%). (C) 2003 Elsevier Ltd. All rights reserved.
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