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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7555-61. doi: 10.1016/j.bmcl.2012.10.022. Epub 2012 Oct 13.

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

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Korea Institute of Science and Technology, 39-1 Hawolgog-dong, Sungbuk-gu, Seoul 136-791, Republic of Korea.


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 Aβ-RAGE binding. SAR studies showed that introducing an amino group at part A was essential for inhibitory activity on Aβ-RAGE binding. Compounds selected from Aβ-RAGE binding screening displayed inhibitory activity on Aβ transport across BBB. They also showed inhibitory activity against Aβ-induced NF-κB activation. These results indicated that our derivatives had a potential as therapeutic agent for the treatment of AD.

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