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6-Phenoxy-2-phenylbenzoxazoles, novel inhibitors of receptor for advanced glycation end products (RAGE)


Year of Publication:
Contact PI Name:
Jeewoo Lee
Contact PI Affiliation:
Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, South Korea
Kwanghyun Choi, Kwang Su Lim, Juhee Shin, Seo Hee Kim, Young-Ger Suh, Hyun-Seok Hong, Hee Kim, Hee-Jin Ha, Young-Ho Kim, Jiyoun Lee
Primary Reference (PubMED ID):
Funding Source:
Korea Science and Engineering Foundation (KOSEF)
Study Goal and Principal Findings:

Receptor for advanced glycation end products (RAGE) is known to be involved in the transportation of amyloid β (Aβ) peptides and causes the accumulation of Aβ in the brain. Moreover, recent studies suggest that the interactions between RAGE and Aβ peptides may be the culprit behind Alzheimer’s disease (AD). Inhibitors of the RAGE–Aβ interactions would not only prevent the accumulation of toxic Aβ in the brain, and but also block the progress of AD, therefore, have the potential to provide a ‘disease-modifying therapy’. In this study, they have developed a series of 6-phenoxy-2-phenylbenzoxazole analogs as novel inhibitors of RAGE. Among these derivatives, they found several effective inhibitors that block the RAGE–Aβ interactions without causing significant cellular toxicity. Further testing showed that compound 48 suppressed Aβ induced toxicity in mouse hippocampal neuronal cells and reduced Aβ levels in the brains of a transgenic mouse model of AD after oral administration.

Therapeutic Agent

Therapeutic Information:
Therapy Type:
Small Molecule
Therapeutic Agent:
Therapeutic Target:
Receptor for Advanced Glycation End Products (RAGE)

Animal Model

Model Information:
Model Type:
Strain/Genetic Background:
Not Reported
Animal Model Notes:
The authors do not specify which APP/PS1 model is used in this study.

Experimental Design

Is the following information reported in the study?:
Power/Sample Size Calculation
Randomized into Groups
Blinded for Treatment
Blinded for Outcome Measures
Pharmacokinetic Measures
Pharmacodynamic Measures
Toxicology Measures
ADME Measures
Route of Delivery
Duration of Treatment
Frequency of Administration
Age of Animal at the Beginning of Treatment
Age of Animal at the End of Treatment
Sex as a Biological Variable
Study Balanced for Sex as a Biological Variable
Number of Premature Deaths
Number of Excluded Animals
Statistical Plan
Genetic Background
Inclusion/Exclusion Criteria Included
Conflict of Interest


Outcome Measured
Outcome Parameters
beta Amyloid Deposits
beta Amyloid Load
Dense-core/Compact Plaques
Brain-beta Amyloid Peptide-Total
Brain-beta Amyloid Peptide 40
Brain-beta Amyloid Peptide 42
Brain-beta Amyloid Deposits
Cell Biology
Cell Viability
Cell Viability