243641-09-0Relevant academic research and scientific papers
Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzheimer's disease
Lee, Yun Suk,Kim, Hee,Kim, Young-Ho,Roh, Eun Joo,Han, Hogyu,Shin, Kye Jung
, p. 7555 - 7561 (2013/02/21)
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.
Efficient synthesis of 1-Benzyloxyphenyl-3-phenylacetones
Mannekens,Tourwe,Lubell
, p. 1214 - 1216 (2007/10/03)
1-[(Benzyloxy)phenyl]-3-phenylacetones 1a-c have been conveniently synthesized by acylation of the PhCH2Li-DABCO complex with their respective N-methyl O-methyl hydroxamates 5a-c. In four steps, ketones 1a-c having ortho-, meta- and para-benzyloxy substituents were obtained in 42-51% overall yields from commercially available 2-(hydroxyphenyl)acetic acids.
