Evidence map›Paper›PMID 29475586›Full record

ArticleBioorganic & medicinal chemistry letters2018

Design and characterization of bivalent compounds as potential neuroprotectants for Alzheimer's disease: Impact of the spacer on biological activity.

Liu He, Ashley Boice, Kai Liu, Xing Yan, Yuqi Jiang, Shijun Zhang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. 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

6 authors.

Liu HeDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA.
Ashley BoiceDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA.
Kai LiuDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA.
Xing YanDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA.
Yuqi JiangDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA.
Shijun ZhangDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA, USA. Electronic address: szhang2@vcu.edu.

Funding

Novel bivalent multifunctional ligands towards Alzheimer's diseaseR01AG041161 · NIA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ZHANG, SHIJUN · 2012 to 2016
$1.5M
NIA NIH HHS R01 AG041161
6 · The paper itself

Abstract

In our continuing efforts to develop bivalent compounds as potential neuroprotectants for Alzheimer's disease, a series of bivalent compounds that contain cholesterylamine and an extended spacer were synthesized and biologically characterized. Our results demonstrated that incorporation of a piperazine ring into the spacer composition significantly improved the protective potency in MC65 cell models. Our results also suggested that the optimal spacer length for such bivalent compounds ranges from 17 to 21 atoms, and further spacer extension beyond 21 atoms results no further optimization. Notably, incorporation of a piperazine ring into the spacer diminished the biometal chelating capacity for these bivalent compounds, thus suggesting structural flexibility of these compounds in interactions with metals. Collectively, the results provided valuable guidance to develop new bivalent compounds as neuroprotectants for Alzheimer's disease.

Indexed as

Drug DesignAlzheimer DiseaseDose-Response Relationship, DrugHumansMolecular StructureNeuroprotective AgentsPiperazinePiperazinesStructure-Activity RelationshipNeuroprotective AgentsPiperazinePiperazinesAlzheimer’s diseaseBivalent compoundsRational designStructural modifications

Identifiers

PMID29475586
PMCPMC5851865

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Registered trials

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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.