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Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-c]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-08-30 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00288 Xiaolin Li 1 , Kai Zhou 1 , Haiying He 1 , Qiong Zhou 1 , Ya Sun 1 , Lijuan Hou 1 , Liang Shen 1 , Xiaofei Wang 1 , Yuedong Zhou 1 , Zhen Gong 1 , Shibo He 1 , Huangtao Jin 1 , Zhengxian Gu 1 , Shuyong Zhao 2 , Long Zhang 2 , Chunyan Sun 2 , Shansong Zheng 2 , Zhe Cheng 2 , Yidong Zhu 2 , Minghui Zhang 2 , Jian Li 1 , Shuhui Chen 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-08-30 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00288 Xiaolin Li 1 , Kai Zhou 1 , Haiying He 1 , Qiong Zhou 1 , Ya Sun 1 , Lijuan Hou 1 , Liang Shen 1 , Xiaofei Wang 1 , Yuedong Zhou 1 , Zhen Gong 1 , Shibo He 1 , Huangtao Jin 1 , Zhengxian Gu 1 , Shuyong Zhao 2 , Long Zhang 2 , Chunyan Sun 2 , Shansong Zheng 2 , Zhe Cheng 2 , Yidong Zhu 2 , Minghui Zhang 2 , Jian Li 1 , Shuhui Chen 1
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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：
四氢吡咯并[1,2-c]嘧啶作为衣壳组装抑制剂用于乙型肝炎治疗的设计、合成和评估
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。构效关系优化产生了一种高效化合物28a (IC 50 = 10 nM)，具有良好的 PK 特性和最受欢迎的 L/P 比。小鼠的水动力注射模型清楚地证明了28a对抗 HBV 复制的功效。
更新日期：2017-08-30
中文翻译：
四氢吡咯并[1,2-c]嘧啶作为衣壳组装抑制剂用于乙型肝炎治疗的设计、合成和评估
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。构效关系优化产生了一种高效化合物28a (IC 50 = 10 nM)，具有良好的 PK 特性和最受欢迎的 L/P 比。小鼠的水动力注射模型清楚地证明了28a对抗 HBV 复制的功效。
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