| Title |
2-acetylphenol analogs as potent reversible monoamine oxidase inhibitors
|
|---|---|
| Published in |
Drug Design, Development and Therapy, July 2015
|
| DOI | 10.2147/dddt.s86225 |
| Pubmed ID | |
| Authors |
Lesetja J Legoabe, Anél Petzer, Jacobus P Petzer |
| Abstract |
Based on a previous report that substituted 2-acetylphenols may be promising leads for the design of novel monoamine oxidase (MAO) inhibitors, a series of C5-substituted 2-acetylphenol analogs (15) and related compounds (two) were synthesized and evaluated as inhibitors of human MAO-A and MAO-B. Generally, the study compounds exhibited inhibitory activities against both MAO-A and MAO-B, with selectivity for the B isoform. Among the compounds evaluated, seven compounds exhibited IC50 values <0.01 µM for MAO-B inhibition, with the most selective compound being 17,000-fold selective for MAO-B over the MAO-A isoform. Analyses of the structure-activity relationships for MAO inhibition show that substitution on the C5 position of the 2-acetylphenol moiety is a requirement for MAO-B inhibition, and the benzyloxy substituent is particularly favorable in this regard. This study concludes that C5-substituted 2-acetylphenol analogs are potent and selective MAO-B inhibitors, appropriate for the design of therapies for neurodegenerative disorders such as Parkinson's disease. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| India | 1 | 50% |
| Unknown | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Scientists | 1 | 50% |
| Practitioners (doctors, other healthcare professionals) | 1 | 50% |
Mendeley readers
The data shown below were compiled from readership statistics for 18 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Germany | 1 | 6% |
| Unknown | 17 | 94% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 6 | 33% |
| Researcher | 3 | 17% |
| Student > Ph. D. Student | 2 | 11% |
| Other | 1 | 6% |
| Lecturer | 1 | 6% |
| Other | 1 | 6% |
| Unknown | 4 | 22% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 3 | 17% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 11% |
| Biochemistry, Genetics and Molecular Biology | 2 | 11% |
| Agricultural and Biological Sciences | 2 | 11% |
| Medicine and Dentistry | 2 | 11% |
| Other | 2 | 11% |
| Unknown | 5 | 28% |
Attention Score in Context
This research output has an Altmetric Attention Score of 2. 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 17 July 2017.
All research outputs
#15,739,529
of 25,373,627 outputs
Outputs from Drug Design, Development and Therapy
#872
of 2,268 outputs
Outputs of similar age
#141,266
of 277,610 outputs
Outputs of similar age from Drug Design, Development and Therapy
#60
of 157 outputs
Altmetric has tracked 25,373,627 research outputs across all sources so far. This one is in the 37th percentile – i.e., 37% of other outputs scored the same or lower than it.
So far Altmetric has tracked 2,268 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.1. This one has gotten more attention than average, scoring higher than 59% 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 277,610 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 47th percentile – i.e., 47% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 157 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 59% of its contemporaries.