| Literature DB >> 28947946 |
Xiaolin Li1, Kai Zhou1, Haiying He1, Qiong Zhou1, Ya Sun1, Lijuan Hou1, Liang Shen1, Xiaofei Wang1, Yuedong Zhou1, Zhen Gong1, Shibo He1, Huangtao Jin1, Zhengxian Gu1, Shuyong Zhao2, Long Zhang2, Chunyan Sun2, Shansong Zheng2, Zhe Cheng2, Yidong Zhu2, Minghui Zhang2, Jian Li1, Shuhui Chen1.
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.Entities:
Keywords: Hepatitis B virus (HBV); capsid assembly inhibitor; tetrahydropyrrolo[1,2-c]pyrimidines
Year: 2017 PMID： 28947946 PMCID： PMC5601373 DOI： 10.1021/acsmedchemlett.7b00288
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345