Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzeheimer's disease

Title
Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzeheimer's disease
Authors
이윤석김희김영호노은주Hogyu Han신계정
Keywords
Alzeheimer's disease; RAGE antagonist; thiazole derivatives; NF-κB; β-Amyloid
Issue Date
2012-12
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 22, NO 24, 7555-7561
Abstract
A series of thiazole derivatives were designed, and prepared to develop RAGE antagonist for the treatment of Alzheimer’s disease (AD). SAR studies were performed to optimize inhibitory activity on Ab- RAGE binding. SAR studies showed that introducing an amino group at part A was essential for inhibitory activity on Ab-RAGE binding. Compounds selected from Ab-RAGE binding screening displayed inhibitory activity on Ab transport across BBB. They also showed inhibitory activity against Ab-induced NF-jB activation. These results indicated that our derivatives had a potential as therapeutic agent for the treatment of AD.
URI
http://pubs.kist.re.kr/handle/201004/44254
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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