| Title |
Inhibitors of Alzheimer’s BACE-1 with 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridine structure
|
|---|---|
| Published in |
Archives of Pharmacal Research, April 2014
|
| DOI | 10.1007/s12272-014-0401-x |
| Pubmed ID | |
| Authors |
Ramin Miri, Omidreza Firuzi, Nima Razzaghi-Asl, Katayoun Javidnia, Najmeh Edraki |
| Abstract |
β-site amyloid precursor protein cleaving enzyme (BACE-1) is a validated target for Alzheimer therapy due to its distinctive role in pathogenesis of AD. In the present contribution, a series of new 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridine structures were synthesized as BACE-1 inhibitors (6a-6n). In vitro BACE-1 inhibitory activities were determined by enzymatic fluorescence resonance energy transfer assay. Synthesized dihydropyridine (DHP) analogues exhibited weak to good inhibitory activities while 6i, 6n and 6a were found to be the most potent molecules with 83.76, 79.45 and 72.47 % BACE-1 inhibition at 10 μM, respectively. Structure binding/activity relationship elucidations revealed that superior BACE-1 inhibitory activities were observed for DHP derivatives bearing fused/non-fused thiazole groups and particularly 3,5-bis-N-(6-ethoxy-2-benzothiazolyl) moiety. Binding maps showed that enhanced activity may be attributed to the additional H-bond and hydrophobic interactions with S2-S3 subpockets of BACE-1. |
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 21 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 1 | 5% |
| Unknown | 20 | 95% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Other | 3 | 14% |
| Student > Doctoral Student | 3 | 14% |
| Researcher | 3 | 14% |
| Student > Master | 3 | 14% |
| Student > Ph. D. Student | 2 | 10% |
| Other | 3 | 14% |
| Unknown | 4 | 19% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 9 | 43% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 10% |
| Physics and Astronomy | 1 | 5% |
| Agricultural and Biological Sciences | 1 | 5% |
| Medicine and Dentistry | 1 | 5% |
| Other | 1 | 5% |
| Unknown | 6 | 29% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. 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 29 April 2014.
All research outputs
#15,299,919
of 22,754,104 outputs
Outputs from Archives of Pharmacal Research
#967
of 1,294 outputs
Outputs of similar age
#133,717
of 226,899 outputs
Outputs of similar age from Archives of Pharmacal Research
#6
of 15 outputs
Altmetric has tracked 22,754,104 research outputs across all sources so far. This one is in the 22nd percentile – i.e., 22% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,294 research outputs from this source. They receive a mean Attention Score of 4.3. This one is in the 21st percentile – i.e., 21% of its peers scored the same or lower than it.
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 226,899 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 31st percentile – i.e., 31% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 15 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 53% of its contemporaries.