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X Demographics
Mendeley readers
Attention Score in Context
| Title |
2‐Aminothiazoles with Improved Pharmacotherapeutic Properties for Treatment of Prion Disease
|
|---|---|
| Published in |
ChemMedChem, March 2013
|
| DOI | 10.1002/cmdc.201300007 |
| Pubmed ID | |
| Authors |
Zhe Li, B. Michael Silber, Satish Rao, Joel R. Gever, Clifford Bryant, Alejandra Gallardo‐Godoy, Elena Dolghih, Kartika Widjaja, Manuel Elepano, Matthew P. Jacobson, Stanley B. Prusiner, Adam R. Renslo |
| Abstract |
Recently, we described the aminothiazole lead (4-biphenyl-4-ylthiazol-2-yl)-(6-methylpyridin-2-yl)-amine (1), which exhibits many desirable properties, including excellent stability in liver microsomes, oral bioavailability of ∼40 %, and high exposure in the brains of mice. Despite its good pharmacokinetic properties, compound 1 exhibited only modest potency in mouse neuroblastoma cells overexpressing the disease-causing prion protein PrP(Sc) . Accordingly, we sought to identify analogues of 1 with improved antiprion potency in ScN2a-cl3 cells while retaining similar or superior properties. Herein we report the discovery of improved lead compounds such as (6-methylpyridin-2-yl)-[4-(4-pyridin-3-yl-phenyl)thiazol-2-yl]amine and cyclopropanecarboxylic acid (4-biphenylthiazol-2-yl)amide, which exhibit brain exposure/EC50 ratios at least tenfold greater than that of compound 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 36 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 36 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 10 | 28% |
| Student > Master | 4 | 11% |
| Professor > Associate Professor | 4 | 11% |
| Professor | 4 | 11% |
| Researcher | 3 | 8% |
| Other | 4 | 11% |
| Unknown | 7 | 19% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 9 | 25% |
| Chemistry | 9 | 25% |
| Agricultural and Biological Sciences | 4 | 11% |
| Medicine and Dentistry | 2 | 6% |
| Computer Science | 1 | 3% |
| Other | 2 | 6% |
| Unknown | 9 | 25% |
Attention Score in Context
This research output has an Altmetric Attention Score of 8. 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 August 2015.
All research outputs
#4,398,662
of 24,641,327 outputs
Outputs from ChemMedChem
#504
of 3,509 outputs
Outputs of similar age
#38,363
of 220,522 outputs
Outputs of similar age from ChemMedChem
#4
of 53 outputs
Altmetric has tracked 24,641,327 research outputs across all sources so far. Compared to these this one has done well and is in the 82nd percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 3,509 research outputs from this source. They receive a mean Attention Score of 4.0. This one has done well, scoring higher than 85% 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 220,522 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 82% of its contemporaries.
We're also able to compare this research output to 53 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.