Evidence map›Paper›PMID 34979256›Full record

ArticleBioorganic & medicinal chemistry letters2022

4-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators.

Nicky Hwang, Haiqun Ban, Shuo Wu, Kelly McGuire, Ellen Hernandez, Junjun Chen, Qiong Zhao, Manasa Suresh, Benjamin Blass, Usha Viswanathan and 6 more

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.8field-weighted citation impact, top 27% 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

2 citing papers in PubMed, 6 citations in OpenAlex.

  1. Article
  2. Article
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

16 authors at 4 institutions in 2 countries.

Nicky HwangBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Haiqun BanBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA; Renji Hospital Affiliated to Shanghai Jiaotong University School of Medicine, 1630 Dongfang Road, Pudong New District, Shanghai 200127, China.
Shuo WuBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Kelly McGuireTemple University, 1801 N Broad St, Philadelphia, PA 191222, USA.
Ellen HernandezDelaware Valley University, 700 E Butler Ave, Doylestown, PA 18901, USA.
Junjun ChenBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Qiong ZhaoBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Manasa SureshGeorgetown University Medical Center, 3900 Reservoir Road, Washington, DC 20057, USA.
Benjamin BlassTemple University School of Pharmacy, Department of Pharmaceutical Sciences 3307 North Broad Street, Philadelphia, PA 19140, USA.
Usha ViswanathanBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
John KulpBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Jinhong ChangBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Jason ClementBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Stephan MenneGeorgetown University Medical Center, 3900 Reservoir Road, Washington, DC 20057, USA.
Ju-Tao GuoBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA. Electronic address: ju-tao.guo@bblumberg.org.
Yanming DuBaruch S. Blumberg Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA. Electronic address: yanming.du@bblumberg.org.
Baruch S. Blumberg Institute · USGeorgetown University · USTemple University · USDelaware Valley College · US

Funding

Evaulation of therapeutic benefits of HBV nucleocapsid assembly inhibitorsR01AI113267 · NIAID · DREXEL UNIVERSITY · PI DU, YANMING, GUO, JU-TAO · 2014 to 2018
$2.9M
NIAID NIH HHS R01 AI113267
6 · The paper itself

Abstract

Hepatitis B virus (HBV) core protein, the building block of the HBV capsid, plays multiple roles in viral replication, and is an attractive target for development of antiviral agents with a new mechanism of action. In addition to the heteroaryldihydropyrimidines (HAPs), sulfamoylbenzamides (SBAs), dibenzothiazepine derivatives (DBTs), and sulfamoylpyrrolamides (SPAs) that inhibit HBV replication by modulation of viral capsid assembly and are currently under clinical trials for the treatment of chronic hepatitis B (CHB), other chemical structures with activity to modulate HBV capsid assembly have also been explored. Here we describe our continued optimization of a benzamide originating from our high throughput screening. A new bicyclic carboxamide lead featuring an electron deficient non-planar core structure was discovered. Evaluations of its ADMET (absorption, distribution, metabolism, excretion and toxicity) and pharmacokinetic (PK) profiles demonstrate improved metabolic stability and good bioavailability.

Indexed as

AnimalsAntiviral AgentsDose-Response Relationship, DrugHepatitis B virusHumansMiceMicrobial Sensitivity TestsMicrosomes, LiverMolecular StructureQuinolinesStructure-Activity RelationshipViral Core ProteinsVirus ReplicationAntiviral AgentsQuinolinesViral Core Proteins4-Oxooctahydroquinoline-1(2H)-carboxamidesCapsid assembly modulatorsHepatitis B virusPhenyl ureas

Identifiers

PMID34979256
PMCPMC8792325
OpenAlexW4205975147

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.