Evidence map›Paper›PMID 32707357›Full record

ArticleEuropean journal of medicinal chemistry2020

Development of coumarine derivatives as potent anti-filovirus entry inhibitors targeting viral glycoprotein.

Yinyi Gao, Han Cheng, Sameer Khan, Gaokeng Xiao, Lijun Rong, Chuan Bai

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.2field-weighted citation impact, top 33% 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

6 citing papers in PubMed, 21 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Ebola Virus Entry Inhibitors.Advances in experimental medicine and biology · 2022
    Article
  5. Article
  6. Trending Topics on Coumarin and Its Derivatives in 2020.Molecules (Basel, Switzerland) · 2021
    Review
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

6 authors at 2 institutions in 2 countries.

Yinyi GaoInstitute of Human Virology, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, Guangdong, 510080, China.
Han ChengDepartment of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, USA.
Sameer KhanDepartment of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, USA.
Gaokeng XiaoGuangzhou Molcalx Information & Technology Ltd, Guangzhou, Guangdong, 510630, China.
Lijun RongDepartment of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, USA. Electronic address: lijun@uic.edu.
Chuan BaiInstitute of Human Virology, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, Guangdong, 510080, China. Electronic address: baichuan@mail.sysu.edu.cn.
University of Illinois Chicago · USSun Yat-sen University · CN

Funding

4-(Aminomethyl) benzamides as novel anti-Ebola agentsR42AI126971 · NIAID · CHICAGO BIOSOLUTIONS, INC. · PI RONG, LIJUN · 2019 to 2021
$2.9M
4-(Aminomethyl) benzamides as novel anti-Ebola agentsR41AI126971 · NIAID · CHICAGO BIOSOLUTIONS, INC. · PI RONG, LIJUN · 2016 to 2017
$727k
NIAID NIH HHS R41 AI126971NIAID NIH HHS R42 AI126971
6 · The paper itself

Abstract

Filoviruses, including Ebolavirus (EBOV), Marburgvirus (MARV) and Cuevavirus, cause hemorrhagic fevers in humans with up to 90% mortality rates. In the 2014-2016 West Africa Ebola epidemic, there are 15,261 laboratory confirmed cases and 11,325 total deaths. The lack of effective vaccines and medicines for the prevention and treatment of filovirus infection in humans stresses the urgency to develop antiviral therapeutics against filovirus-associated diseases. Our previous study identified a histamine receptor antagonist compound CP19 as an entry inhibitor against both EBOV and MARV. The preliminary structure-activity relationship (SAR) studies of CP19 showed that its piperidine, coumarin and linker were related with its antiviral activities. In this study, we performed detailed SAR studies on these groups with synthesized CP19 derivatives. We discovered that 1) the piperidine group could be optimized with heterocycles, 2) the substitution groups of C3 and C4 of coumarin should be relatively large hydrophobic groups and 3) the linker part should be least substituted. Based on the SAR analysis, we synthesized compound 32 as a potent entry inhibitor of EBOV and MARV (IC

Indexed as

Drug DesignAntiviral AgentsCoumarinsFiloviridaeMolecular Targeted TherapyPiperidinesStructure-Activity RelationshipViral Envelope ProteinsVirus InternalizationAntiviral AgentsCoumarinspiperidinePiperidinesViral Envelope Proteins

Identifiers

PMID32707357
PMCPMC7529935
OpenAlexW3040953115

What OpenQuestion holds

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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.