TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC 50 value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7 , thereby inducing the secretion of TLR7 -regulated cytokines IL-12 , TNF-αand IFN-αin human PBMC cells. TLR7 agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents.