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Attention Score in Context
| Title |
2-Benzoyl-6-benzylidenecyclohexanone analogs as potent dual inhibitors of acetylcholinesterase and butyrylcholinesterase
|
|---|---|
| Published in |
Bioorganic & Medicinal Chemistry, June 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. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 41 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 41 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 10 | 24% |
| Student > Master | 9 | 22% |
| Professor | 2 | 5% |
| Other | 2 | 5% |
| Student > Ph. D. Student | 2 | 5% |
| Other | 6 | 15% |
| Unknown | 10 | 24% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 12 | 29% |
| Biochemistry, Genetics and Molecular Biology | 6 | 15% |
| Pharmacology, Toxicology and Pharmaceutical Science | 3 | 7% |
| Unspecified | 1 | 2% |
| Arts and Humanities | 1 | 2% |
| Other | 4 | 10% |
| Unknown | 14 | 34% |
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
#3,415,054
of 25,373,627 outputs
Outputs from Bioorganic & Medicinal Chemistry
#415
of 7,493 outputs
Outputs of similar age
#57,753
of 357,327 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry
#7
of 94 outputs
Altmetric has tracked 25,373,627 research outputs across all sources so far. Compared to these this one has done well and is in the 86th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 7,493 research outputs from this source. They receive a mean Attention Score of 4.8. This one has done particularly well, scoring higher than 93% 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 357,327 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 83% of its contemporaries.
We're also able to compare this research output to 94 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 92% of its contemporaries.