Literature DB >> 33421915

Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents.

Franck Amblard1, Sebastien Boucle1, Leda Bassit1, Zhe Chen1, Ozkan Sari1, Bryan Cox1, Kiran Verma1, Tugba Ozturk1, Olivia Ollinger-Russell1, Raymond F Schinazi2.   

Abstract

Chronic hepatitis B viral infection is a significant health problem world-wide, and currently available antiviral agents suppress HBV infections, but rarely cure this disease. It is presumed that antiviral agents that target the viral nuclear reservoir of transcriptionally active cccDNA may eliminate HBV infection. Through a series of chemical optimization, we identified a new series of glyoxamide derivatives affecting HBV nucleocapsid formation and cccDNA maintenance at low nanomolar levels. Among all the compounds synthesized, GLP-26 displays a major effect on HBV DNA, HBeAg secretion and cccDNA amplification. In addition, GLP-26 shows a promising pre-clinical profile and long-term effect on viral loads in a humanized mouse model.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antiviral; Capsid; Hepatitis B virus; cccDNA

Mesh：

Substances：

Year:  2020        PMID： 33421915      PMCID： PMC7856252          DOI： 10.1016/j.bmc.2020.115952

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  10 in total

1.  Inducible expression of human hepatitis B virus (HBV) in stably transfected hepatoblastoma cells: a novel system for screening potential inhibitors of HBV replication.

Authors:  S K Ladner; M J Otto; C S Barker; K Zaifert; G H Wang; J T Guo; C Seeger; R W King
Journal:  Antimicrob Agents Chemother       Date:  1997-08       Impact factor: 5.191

Review 2.  Recent advances in the development of HBV capsid assembly modulators.

Authors:  Bhavitavya Nijampatnam; Dennis C Liotta
Journal:  Curr Opin Chem Biol       Date:  2019-04-02       Impact factor: 8.822

3.  Antiviral activities and cellular toxicities of modified 2',3'-dideoxy-2',3'-didehydrocytidine analogues.

Authors:  Lieven J Stuyver; Stefania Lostia; Marjorie Adams; Judy S Mathew; Balakrishna S Pai; Jason Grier; Phillip M Tharnish; Yongseok Choi; Youhoon Chong; Hyunah Choo; Chung K Chu; Michael J Otto; Raymond F Schinazi
Journal:  Antimicrob Agents Chemother       Date:  2002-12       Impact factor: 5.191

4.  Preclinical characterization of GLS4, an inhibitor of hepatitis B virus core particle assembly.

Authors:  Guoyi Wu; Bo Liu; Yingjun Zhang; Jing Li; Alla Arzumanyan; Marcia M Clayton; Raymond F Schinazi; Zhaohe Wang; Siegfried Goldmann; Qingyun Ren; Faxhou Zhang; Mark A Feitelson
Journal:  Antimicrob Agents Chemother       Date:  2013-08-19       Impact factor: 5.191

5.  Development of a quantitative real-time detection assay for hepatitis B virus DNA and comparison with two commercial assays.

Authors:  S D Pas; E Fries; R A De Man; A D Osterhaus; H G Niesters
Journal:  J Clin Microbiol       Date:  2000-08       Impact factor: 5.948

6.  Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.

Authors:  Ozkan Sari; Sebastien Boucle; Bryan D Cox; Tugba Ozturk; Olivia Ollinger Russell; Leda Bassit; Franck Amblard; Raymond F Schinazi
Journal:  Eur J Med Chem       Date:  2017-06-29       Impact factor: 6.514

7.  Antiviral Properties and Mechanism of Action Studies of the Hepatitis B Virus Capsid Assembly Modulator JNJ-56136379.

Authors:  Jan Martin Berke; Pascale Dehertogh; Karen Vergauwen; Wendy Mostmans; Koen Vandyck; Pierre Raboisson; Frederik Pauwels
Journal:  Antimicrob Agents Chemother       Date:  2020-04-21       Impact factor: 5.191

8.  Novel Hepatitis B Virus Capsid Assembly Modulator Induces Potent Antiviral Responses In Vitro and in Humanized Mice.

Authors:  Franck Amblard; Sebastien Boucle; Leda Bassit; Bryan Cox; Ozkan Sari; Sijia Tao; Zhe Chen; Tugba Ozturk; Kiran Verma; Olivia Russell; Virgile Rat; Hugues de Rocquigny; Oriane Fiquet; Maud Boussand; James Di Santo; Helene Strick-Marchand; Raymond F Schinazi
Journal:  Antimicrob Agents Chemother       Date:  2020-01-27       Impact factor: 5.191

9.  Safety, pharmacokinetics, and antiviral effects of ABI-H0731, a hepatitis B virus core inhibitor: a randomised, placebo-controlled phase 1 trial.

Authors:  Man-Fung Yuen; Kosh Agarwal; Edward J Gane; Christian Schwabe; Sang Hoon Ahn; Dong Joon Kim; Young-Suk Lim; Wendy Cheng; William Sievert; Kumar Visvanathan; Eric Ruby; Sandy Liaw; Ran Yan; Qi Huang; Richard Colonno; Uri Lopatin
Journal:  Lancet Gastroenterol Hepatol       Date:  2019-11-09

10.  Heteroaryldihydropyrimidine (HAP) and Sulfamoylbenzamide (SBA) Inhibit Hepatitis B Virus Replication by Different Molecular Mechanisms.

Authors:  Zheng Zhou; Taishan Hu; Xue Zhou; Steffen Wildum; Fernando Garcia-Alcalde; Zhiheng Xu; Daitze Wu; Yi Mao; Xiaojun Tian; Yuan Zhou; Fang Shen; Zhisen Zhang; Guozhi Tang; Isabel Najera; Guang Yang; Hong C Shen; John A T Young; Ning Qin
Journal:  Sci Rep       Date:  2017-02-13       Impact factor: 4.379
  10 in total
  2 in total

1.  The Mechanism of Action of Hepatitis B Virus Capsid Assembly Modulators Can Be Predicted from Binding to Early Assembly Intermediates.

Authors:  Anna Pavlova; Leda Bassit; Bryan D Cox; Maksym Korablyov; Christophe Chipot; Dharmeshkumar Patel; Diane L Lynch; Franck Amblard; Raymond F Schinazi; James C Gumbart
Journal:  J Med Chem       Date:  2022-03-15       Impact factor: 8.039

2.  Assessment of a Computational Approach to Predict Drug Resistance Mutations for HIV, HBV and SARS-CoV-2.

Authors:  Dharmeshkumar Patel; Suzane K Ono; Leda Bassit; Kiran Verma; Franck Amblard; Raymond F Schinazi
Journal:  Molecules       Date:  2022-08-24       Impact factor: 4.927
  2 in total

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