1 research outputs found
Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2‑<i>c</i>]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment
The discovery of
novel tetrahydropyrroloÂ[1,2-<i>c</i>]Âpyrimidines derivatives
from <b>Bay41_4109</b> as hepatitis
B virus (HBV) inhibitors is herein reported. The structure–activity
relationship optimization led to one highly efficacious compound <b>28a</b> (IC<sub>50</sub> = 10 nM) with good PK profiles and the
favorite L/P ratio. The hydrodynamic injection model in mice clearly
demonstrated the efficacy of <b>28a</b> against HBV replication