Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzeheimer's disease
- Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzeheimer's disease
- 이윤석; 김희; 김영호; 노은주; Hogyu Han; 신계정
- Alzeheimer's disease; RAGE antagonist; thiazole derivatives; NF-κB; β-Amyloid
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 22, NO 24, 7555-7561
- 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
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