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Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzheimer's disease
- Issue Date
- 15-12월-2012
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Alzheimer' s disease; RAGE antagonist; NF-kappa B; beta-Amyloid
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.24, pp.7555 - 7561
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 22
- Number
- 24
- Start Page
- 7555
- End Page
- 7561
- ISSN
- 0960-894X
- 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 A beta-RAGE binding. SAR studies showed that introducing an amino group at part A was essential for inhibitory activity on A beta-RAGE binding. Compounds selected from A beta-RAGE binding screening displayed inhibitory activity on A beta transport across BBB. They also showed inhibitory activity against A beta-induced NF-kappa B activation. These results indicated that our derivatives had a potential as therapeutic agent for the treatment of AD. (C) 2012 Elsevier Ltd. All rights reserved.
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