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This chapter summarizes selected small‐molecule Toll‐like receptor 7 (TLR‐7) agonists that have been developed for viral hepatitis infections. An introduction to the rationale for TLR‐7 as a target for HCV and HBV is presented. The initial discovery of interferon inducers that were later found to be TLR‐7 agonists, and how they led to the initiation of drug discovery programs, are also described. The primary focus is a summary of the characteristics and structure–activity relationships in each of the major classes of agonists that have advanced into development and also findings in clinical trials for hepatitis C infection where available. Finally, an outlook for this class of compounds for the treatment of hepatitis B and C is presented.

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