Evidence map›Paper›PMID 28688280›Full record

ArticleEuropean journal of medicinal chemistry2017

Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.

Ozkan Sari, Sebastien Boucle, Bryan D Cox, Tugba Ozturk, Olivia Ollinger Russell, Leda Bassit, Franck Amblard, Raymond F Schinazi

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
4.3field-weighted citation impact, top 5% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

16 citing papers in PubMed, 46 citations in OpenAlex.

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  7. Site-Selective C-H Arylation of Diverse Arenes Ortho to Small Alkyl Groups.Angewandte Chemie (International ed. in English) · 2022
    Article
  8. Article
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  11. Synthesis of 4-oxotetrahydropyrimidine-1(2H)-carboxamides derivatives as capsid assembly modulators of hepatitis B virus.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021
    Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 1 institution in 1 country.

Ozkan SariCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Sebastien BoucleCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Bryan D CoxCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Tugba OzturkCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Olivia Ollinger RussellCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Leda BassitCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Franck AmblardCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Raymond F SchinaziCenter for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. Electronic address: rschina@emory.edu.
Emory University · US

Funding

Virology and Molecular Biomarkers CoreP30AI050409 · NIAID · EMORY UNIVERSITY · PI Ann M Chahroudi, Colleen F Kelley · 2002 to 2026
$74.0M
HBV Capsid EffectorsR01AI132833 · NIAID · EMORY UNIVERSITY · PI Raymond Felix Schinazi · 2017 to 2026
$5.3M
NIAID NIH HHS P30 AI050409NIAID NIH HHS R01 AI132833
6 · The paper itself

Abstract

The synthesis of novel series of sulfamoylbenzamides as HBV capsid assembly effector is reported. The structure was divided into five parts which were independently modified as part of our lead optimization. All synthesized compounds were evaluated for their anti-HBV activity and toxicity in human hepatocytes, lymphocytes and other cells. Additionally, we assessed their effect on HBV cccDNA formation in an HBeAg reporter cell-based assay. Among the 27 compounds reported, several analogs exhibited submicromolar activities and significant reduction of HBeAg secretion. Selected compounds were studied under negative-stain electron microscopy for their ability to disrupt the HBV capsid formation. Structures were modeled into a binding site recently identified in the HBV capsid protein for similar molecules to rationalize the structure-activity relationships for this family of compounds.

Indexed as

AnimalsAntiviral AgentsBenzamidesCapsidCell ProliferationCells, CulturedChlorocebus aethiopsDose-Response Relationship, DrugHepatitis B virusHumansMicrobial Sensitivity TestsModels, MolecularMolecular StructureStructure-Activity RelationshipVero CellsVirus AssemblyAntiviral AgentsBenzamidesAntiviral agentCapsid assembly effectorcccDNAHBeAgHBVSulfamoylbenzamide

Identifiers

PMID28688280
PMCPMC5581232
OpenAlexW2729133950

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.