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Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-c]pyrimidines as Capsid Assembly Inhibitors for HBV Treatment
- Source :
- ACS Medicinal Chemistry Letters. 8:969-974
- Publication Year :
- 2017
- Publisher :
- American Chemical Society (ACS), 2017.
-
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.
- Subjects :
- 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
Subjects
Details
- ISSN :
- 19485875
- Volume :
- 8
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....eb712d1a0e524f5e9b477c6ba9afb2a8