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Cited by 82Cholinesterase and Neurodegenerative DiseasesHeterocyclic Compound Synthesis and BioactivityAlzheimer's disease research and treatments

The DOI matches its Crossref record; 28 of the 31 references it cites were found in a registry or an index.

Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies

Abstract

The synthesis of novel indolopyrazoline derivatives (P1-P4 and Q1-Q4) has been characterized and evaluated as potential anti-Alzheimer agents through in vitro Acetylcholinesterase (AChE) inhibition and radical scavenging activity (antioxidant) studies. Specifically, Q3 shows AChE inhibition (IC50: 0.68±0.13μM) with strong DPPH and ABTS radical scavenging activity (IC50: 13.77±0.25μM and IC50: 12.59±0.21μM), respectively. While P3 exhibited as the second most potent compound with AChE inhibition (IC50: 0.74±0.09μM) and with DPPH and ABTS radical scavenging activity (IC50: 13.52±0.62μM and IC50: 13.13±0.85μM), respectively. Finally, molecular docking studies provided prospective evidence to identify key interactions between the active inhibitors and the AChE that furthermore led us to the identification of plausible binding mode of novel indolopyrazoline derivatives. Additionally, in-silico ADME prediction using QikProp shows that these derivatives fulfilled all the properties of CNS acting drugs. This study confirms the first time reporting of indolopyrazoline derivatives as potential anti-Alzheimer agents.

Overview

Integrity signals

Registry

Crossref · 10.1016/j.bioorg.2016.05.002

Cites

28 of 28 references verified0 citation errors · 0 not checkable

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Citations

Cites

Research works printed but not linked: 3

  1. Sridevi, 2009, Antioxidant and antiinflammatory activity of some phenylpyrazolo benzimidazolo quinoxaline derivatives, J. Pharm. Res., 2, 1370
  2. Suthakaran, 2007, Synthesis, antiinflammatory, antioxidant and antibacterial activities of 7-methoxy benzofuran pyrazoline derivatives, Asian J. Chem., 19, 3353
  3. Sridevi, 2009, Antioxidant, antiinflammatory and antihistaminic activities of some phenylpyrazolo benzothiazolo quinoxaline derivatives, Int. J. Chem. Sci., 7, 1117

Cited by

See all 82

Metadata

Authors
Chigurupati, S., Selvaraj, M., Mani, V., Selvarajan, K. K., Mohammad, J. I., Kaveti, B., Bera, H., Palanimuthu, V. R., Teh, L. K., & Salleh, M. Z.
Affiliations
  • AIMST University (MY)
  • Universiti Teknologi MARA System (MY)
  • Qassim University (SA)
Corresponding author
  • Chigurupati, Sridevi
  • Selvaraj, Manikandan
Venue
Bioorganic Chemistry
Publisher
Elsevier BV
Published
2016-08
Volume
67
Pages
9-17
ISSN
0045-2068 (ISSN-L)
OpenAlex
W2388623795
Cited by
82
References
31
Citations by year
2026: 5 · 2025: 4 · 2024: 12 · 2023: 11 · 2022: 14 · 2021: 11 · 2020: 6 · 2019: 6 · 2018: 6 · 2017: 7
FWCI
5.13
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Bioorganic Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • Research Portal (Queen's University Belfast) (submittedVersion)
Funders
Ministry of Higher Education, Malaysia (600-RMI/TRGS 5/3 (1/2014)-3)
Topics
  • Health Sciences › Medicine › Pharmacology (medical) › Cholinesterase and Neurodegenerative Diseases
  • Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
Keywords
acetylcholinesterase inhibitors, anti-Alzheimer agents, Alzheimer's disease, antioxidant activity, free radical scavenging, DPPH radical, ABTS radical, molecular docking, ADME prediction, CNS drug candidates
MeSH terms
Acetylcholinesterase, Antioxidants, Cholinesterase Inhibitors, Dose-Response Relationship, Drug, Humans, Indoles, Pyrazoles, Structure-Activity Relationship, Molecular Structure, Molecular Docking Simulation

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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

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Data sources

Bibliographic data: Semantic Scholar, OpenAlex, Crossref.

Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.