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Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand

Overview of attention for article published in Bioorganic & Medicinal Chemistry Letters, June 2018
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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 (80th percentile)
  • High Attention Score compared to outputs of the same age and source (95th percentile)

Mentioned by

news
1 news outlet
twitter
1 X user

Citations

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3 Dimensions

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21 Mendeley
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Title
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand
Published in
Bioorganic & Medicinal Chemistry Letters, June 2018
DOI 10.1016/j.bmcl.2018.06.045
Pubmed ID
Authors

Arun K Ghosh, Koena Ghosh, Margherita Brindisi, Emma K Lendy, Yu-Chen Yen, Nagaswamy Kumaragurubaran, Xiangping Huang, Jordan Tang, Andrew D Mesecar

Abstract

We describe the design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors containing bicyclic isoxazoline carboxamides as the P3 ligand in combination with methyl cysteine, methylsulfonylalanine and Boc-amino alanine as P2 ligands. Inhibitor 3a displayed a BACE1 Ki value of 10.9 nM and EC50 of 343 nM. The X-ray structure of 3a bound to the active site of BACE1 was determined at 2.85 Å resolution. The structure revealed that the major molecular interactions between BACE1 and the bicyclic tetrahydrofuranyl isoxazoline heterocycle are van der Waals in nature.

X Demographics

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.
Mendeley readers

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 %
Unknown 21 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 3 14%
Researcher 2 10%
Student > Ph. D. Student 2 10%
Other 1 5%
Student > Doctoral Student 1 5%
Other 2 10%
Unknown 10 48%
Readers by discipline Count As %
Chemistry 6 29%
Biochemistry, Genetics and Molecular Biology 2 10%
Pharmacology, Toxicology and Pharmaceutical Science 2 10%
Unknown 11 52%
Attention Score in Context

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 16 September 2018.
All research outputs
#3,417,018
of 25,385,509 outputs
Outputs from Bioorganic & Medicinal Chemistry Letters
#827
of 13,783 outputs
Outputs of similar age
#65,745
of 342,601 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry Letters
#3
of 65 outputs
Altmetric has tracked 25,385,509 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 13,783 research outputs from this source. They receive a mean Attention Score of 4.9. 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 342,601 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 80% of its contemporaries.
We're also able to compare this research output to 65 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 95% of its contemporaries.