Design and Synthesis of Novel 5-Substituted Acyclic Pyrimidine Nucleosides as Potent and Selective Inhibitors of Hepatitis B Virus

2002 ◽  
Vol 45 (10) ◽  
pp. 2032-2040 ◽  
Author(s):  
Rakesh Kumar ◽  
Mahendra Nath ◽  
D. Lorne J. Tyrrell
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Selective Inhibitors ◽  
Pyrimidine Nucleosides ◽  
Design And Synthesis ◽  
B Virus

scholarly journals Pure nucleoside enantiomers of beta-2',3'-dideoxycytidine analogs are selective inhibitors of hepatitis B virus in vitro.

1994 ◽  
Vol 38 (9) ◽  
pp. 2172-2174 ◽  
Author(s):  
R F Schinazi ◽  
G Gosselin ◽  
A Faraj ◽  
B E Korba ◽  
D C Liotta ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Selective Inhibitors ◽  
B Virus ◽  
Beta 2

Selective Inhibitors of Hepatitis B Virus Replication

2003 ◽  
Vol 2 (3) ◽  
pp. 227-240 ◽  
Author(s):  
Chunxiao Ying ◽  
Erik Clercq ◽  
Johan Neyts
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Virus Replication ◽  
Selective Inhibitors ◽  
B Virus

Rational Design and Synthesis of 2,2-Bisheterocycle Tandem Derivatives as Non-Nucleoside Hepatitis B Virus Inhibitors

ChemMedChem ◽  
2008 ◽  
Vol 3 (9) ◽  
pp. 1316-1321 ◽  
Author(s):  
Hai-Jun Chen ◽  
Wen-Long Wang ◽  
Gui-Feng Wang ◽  
Li-Ping Shi ◽  
Min Gu ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Rational Design ◽  
Design And Synthesis ◽  
B Virus

Design and Synthesis of Oxymatrine Analogues Overcoming Drug Resistance in Hepatitis B Virus through Targeting Host Heat Stress Cognate 70

2011 ◽  
Vol 54 (3) ◽  
pp. 869-876 ◽  
Author(s):  
Li-Mei Gao ◽  
Yan-Xing Han ◽  
Yu-Ping Wang ◽  
Yu-Huan Li ◽  
Yong-Qiang Shan ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Heat Stress ◽  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Design And Synthesis ◽  
B Virus

Structure−Activity Relationships of 1-(2-Deoxy-2-fluoro-β-l-arabino- furanosyl)pyrimidine Nucleosides as Anti-Hepatitis B Virus Agents

1996 ◽  
Vol 39 (14) ◽  
pp. 2835-2843 ◽  
Author(s):  
Tianwei Ma ◽  
S. Balakrishna Pai ◽  
Yong Lian Zhu ◽  
Ju Sheng Lin ◽  
Kirupa Shanmuganathan ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Pyrimidine Nucleosides ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
B Virus

scholarly journals Discovery of New Small Molecule Hits as Hepatitis B Virus Capsid Assembly Modulators: Structure and Pharmacophore-Based Approaches

Viruses ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 770
Author(s):  
Sameera Senaweera ◽  
Haijuan Du ◽  
Huanchun Zhang ◽  
Karen A. Kirby ◽  
Philip R. Tedbury ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Small Molecule ◽  
Capsid Assembly ◽  
Single Digit ◽  
Protein Protein Interaction ◽  
Design And Synthesis ◽  
B Virus ◽  
Preclinical And Clinical Studies ◽  
Thermal Shift

Hepatitis B virus (HBV) capsid assembly modulators (CpAMs) have shown promise as potent anti-HBV agents in both preclinical and clinical studies. Herein, we report our efforts in identifying novel CpAM hits via a structure-based virtual screening against a small molecule protein-protein interaction (PPI) library, and pharmacophore-guided compound design and synthesis. Curated compounds were first assessed in a thermal shift assay (TSA), and the TSA hits were further evaluated in an antiviral assay. These efforts led to the discovery of two structurally distinct scaffolds, ZW-1841 and ZW-1847, as novel HBV CpAM hits, both inhibiting HBV in single-digit µM concentrations without cytotoxicity at 100 µM. In ADME assays, both hits displayed extraordinary plasma and microsomal stability. Molecular modeling suggests that these hits bind to the Cp dimer interfaces in a mode well aligned with known CpAMs.

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