Evidence map›Paper›PMID 28274151›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2017

Pharmacophore-based design and discovery of (-)-meptazinol carbamates as dual modulators of cholinesterase and amyloidogenesis.

Qiong Xie, Zhaoxi Zheng, Biyun Shao, Wei Fu, Zheng Xia, Wei Li, Jian Sun, Wei Zheng, Weiwei Zhang, Wei Sheng and 4 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Novel Sulfonamide-Based Carbamates as Selective Inhibitors of BChE.International journal of molecular sciences · 2021
    Article
  3. 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

14 authors.

Qiong Xiea Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Zhaoxi Zhengb Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Biyun Shaob Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Wei Fua Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Zheng Xiab Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Wei Lia Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Jian Suna Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Wei Zhenga Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Weiwei Zhangb Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Wei Shenga Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Qihong Zhanga Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.
Hongzhuan Chenb Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Hao Wangb Department of Pharmacology , Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine , Shanghai , P. R. China.
Zhuibai Qiua Department of Medicinal Chemistry , School of Pharmacy, Fudan University , Shanghai , P. R. China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Multifunctional carbamate-type acetylcholinesterase (AChE) inhibitors with anti-amyloidogenic properties like phenserine are potential therapeutic agents for Alzheimer's disease (AD). We reported here the design of new carbamates using pharmacophore model strategy to modulate both cholinesterase and amyloidogenesis. A five-feature pharmacophore model was generated based on 25 carbamate-type training set compounds. (-)-Meptazinol carbamates that superimposed well upon the model were designed and synthesized, which exhibited nanomolar AChE inhibitory potency and good anti-amyloidogenic properties in in vitro test. The phenylcarbamate 43 was highly potent (IC

Indexed as

Drug DiscoveryAmyloidAnimalsCarbamatesCholinesterase InhibitorsCholinesterasesDose-Response Relationship, DrugEnzyme-Linked Immunosorbent AssayFemaleHumansKineticsMaleMeptazinolMiceMice, Inbred StrainsModels, MolecularAmyloidCarbamatesCholinesterase InhibitorsCholinesterasesMeptazinolacetylcholinesteraseamyloidogenesiscarbamates(−)-meptazinolPharmacophore

Identifiers

PMID28274151
PMCPMC6009976

What OpenQuestion holds

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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.