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Structure-Based Design, Synthesis, Biological Evaluation, and Molecular Docking of Novel PDE10 Inhibitors With Antioxidant Activities

Overview of attention for article published in Frontiers in Chemistry, May 2018
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Title
Structure-Based Design, Synthesis, Biological Evaluation, and Molecular Docking of Novel PDE10 Inhibitors With Antioxidant Activities
Published in
Frontiers in Chemistry, May 2018
DOI 10.3389/fchem.2018.00167
Pubmed ID
Authors

Jinxuan Li, Jing-Yi Chen, Ya-Lin Deng, Qian Zhou, Yinuo Wu, Deyan Wu, Hai-Bin Luo

Abstract

Phosphodiesterase 10 is a promising target for the treatment of a series of central nervous system (CNS) diseases. Imbalance between oxidative stress and antioxidant defense systems as a universal condition in neurodegenerative disorders is widely studied as a potential therapy for CNS diseases, such as Alzheimer's disease (AD), Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS). To discover multifunctional pharmaceuticals as a treatment for neurodegenerative diseases, a series of quinazoline-based derivatives with PDE10 inhibitory activities and antioxidant activities were designed and synthesized. Nine out of 13 designed compounds showed good PDE10 inhibition at the concentration of 1.0 μM. Among these compounds, eight exhibited moderate to excellent antioxidant activity with ORAC (oxygen radical absorbance capacity) value above 1.0. Molecular docking was performed for better understanding of the binding patterns of these compounds with PDE10. Compound 11e, which showed remarkable inhibitory activity against PDE10 and antioxidant activity may serve as a lead for the further modification.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 24 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 24 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 4 17%
Student > Master 4 17%
Researcher 3 13%
Student > Bachelor 2 8%
Student > Doctoral Student 1 4%
Other 3 13%
Unknown 7 29%
Readers by discipline Count As %
Chemistry 5 21%
Pharmacology, Toxicology and Pharmaceutical Science 2 8%
Biochemistry, Genetics and Molecular Biology 2 8%
Neuroscience 2 8%
Psychology 1 4%
Other 3 13%
Unknown 9 38%
Attention Score in Context

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 15 May 2018.
All research outputs
#20,490,710
of 23,054,359 outputs
Outputs from Frontiers in Chemistry
#2,938
of 6,022 outputs
Outputs of similar age
#287,327
of 326,931 outputs
Outputs of similar age from Frontiers in Chemistry
#82
of 163 outputs
Altmetric has tracked 23,054,359 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,022 research outputs from this source. They receive a mean Attention Score of 2.0. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 163 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.