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2-Benzoyl-6-benzylidenecyclohexanone analogs as potent dual inhibitors of acetylcholinesterase and butyrylcholinesterase

Overview of attention for article published in Bioorganic & Medicinal Chemistry, August 2016
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (84th percentile)
  • High Attention Score compared to outputs of the same age and source (96th percentile)

Mentioned by

news
1 news outlet
twitter
1 tweeter

Citations

dimensions_citation
9 Dimensions

Readers on

mendeley
33 Mendeley
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Title
2-Benzoyl-6-benzylidenecyclohexanone analogs as potent dual inhibitors of acetylcholinesterase and butyrylcholinesterase
Published in
Bioorganic & Medicinal Chemistry, August 2016
DOI 10.1016/j.bmc.2016.06.016
Pubmed ID
Authors

Sze Wei Leong, Faridah Abas, Kok Wai Lam, Khozirah Shaari, Nordin H. Lajis

Abstract

In the present study, a series of 2-benzoyl-6-benzylidenecyclohexanone analogs have been synthesized and evaluated for their anti-cholinesterase activity. Among the forty-one analogs, four compounds (38, 39, 40 and 41) have been identified as lead compounds due to their highest inhibition on both AChE and BChE activities. Compounds 39 and 40 in particular exhibited highest inhibition on both AChE and BChE with IC50 values of 1.6μM and 0.6μM, respectively. Further structure-activity relationship study suggested that presence of a long-chain heterocyclic in one of the rings played a critical role in the dual enzymes' inhibition. The Lineweaver-Burk plots and docking results suggest that both compounds could simultaneously bind to the PAS and CAS regions of the enzyme. ADMET analysis further confirmed the therapeutic potential of both compounds based upon their high BBB-penetrating. Thus, 2-benzoyl-6-benzylidenecyclohexanone containing long-chain heterocyclic amine analogs represent a new class of cholinesterase inhibitor, which deserve further investigation for their development into therapeutic agents for cognitive diseases such as Alzheimer.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 33 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 33 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 7 21%
Student > Bachelor 6 18%
Unspecified 4 12%
Professor 2 6%
Student > Ph. D. Student 2 6%
Other 7 21%
Unknown 5 15%
Readers by discipline Count As %
Chemistry 10 30%
Biochemistry, Genetics and Molecular Biology 4 12%
Unspecified 4 12%
Pharmacology, Toxicology and Pharmaceutical Science 2 6%
Agricultural and Biological Sciences 1 3%
Other 2 6%
Unknown 10 30%

Attention Score in Context

This research output has an Altmetric Attention Score of 10. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 02 July 2016.
All research outputs
#1,265,015
of 12,272,194 outputs
Outputs from Bioorganic & Medicinal Chemistry
#104
of 5,113 outputs
Outputs of similar age
#40,106
of 270,936 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry
#2
of 82 outputs
Altmetric has tracked 12,272,194 research outputs across all sources so far. Compared to these this one has done well and is in the 89th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 5,113 research outputs from this source. They receive a mean Attention Score of 4.0. This one has done particularly well, scoring higher than 97% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 270,936 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 84% of its contemporaries.
We're also able to compare this research output to 82 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 96% of its contemporaries.