Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-c]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment
| Autor: | Zhen Gong, Huangtao Jin, Lijuan Hou, Cheng Zhe, Chen Shuhui, Haiying He, Yidong Zhu, Zhang Long, Liang Shen, Yuedong Zhou, Zhao Shuyong, Wang Xiaofei, Zheng Shansong, Ya Sun, Kai Zhou, Jian Li, Zhengxian Gu, Qiong Zhou, Shibo He, Li Xiaolin, Minghui Zhang, Chunyan Sun |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Hepatitis B virus Chemistry Organic Chemistry medicine.disease_cause Hbv replication Biochemistry Virology 03 medical and health sciences 030104 developmental biology 0302 clinical medicine Capsid Design synthesis Drug Discovery medicine Hepatitis B virus HBV 030211 gastroenterology & hepatology IC50 |
| Zdroj: | ACS Medicinal Chemistry Letters. 8:969-974 |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.7b00288 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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