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Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-c]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment.


ABSTRACT: 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.

SUBMITTER: Li X 

PROVIDER: S-EPMC5601373 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-<i>c</i>]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment.

Li Xiaolin X   Zhou Kai K   He Haiying H   Zhou Qiong Q   Sun Ya Y   Hou Lijuan L   Shen Liang L   Wang Xiaofei X   Zhou Yuedong Y   Gong Zhen Z   He Shibo S   Jin Huangtao H   Gu Zhengxian Z   Zhao Shuyong S   Zhang Long L   Sun Chunyan C   Zheng Shansong S   Cheng Zhe Z   Zhu Yidong Y   Zhang Minghui M   Li Jian J   Chen Shuhui S  

ACS medicinal chemistry letters 20170824 9


The discovery of novel tetrahydropyrrolo[1,2-<i>c</i>]pyrimidines 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. ...[more]

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