The discovery of novel tetrahydropyrrolo[1,2-c]pyrimidines derivatives from Bay41_4109 as hepatitis B virus (HBV) inhibitors is herein reported. The structure–activity relationship optimization led to one highly efficacious compound 28a (IC₅₀ = 10 nM) with good PK profiles and the favorite L/P ratio. The hydrodynamic injection model in mice clearly demonstrated the efficacy of 28a against HBV replication.

中文翻译：

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设计，合成和评估四氢吡咯并[1,2- c ]嘧啶类药物作为用于HBV治疗的衣壳装配抑制剂

本文报道了来自Bay41_4109的新型四氢吡咯并[1,2- c ]嘧啶衍生物作为乙型肝炎病毒（HBV）抑制剂的发现。通过结构-活性关系优化，得到了一种高效化合物28a（IC ₅₀ = 10 nM），具有良好的PK分布和最佳的L / P比。小鼠体内的流体动力注射模型清楚地证明了28a对抗HBV复制的功效。