Synthesis of Functionalized Benzoxazoles and Their Binding Affinities to A¥â42 Fibrils

Bulletin of the Korean chemical society

Young Shin Chun¹  Kyung Ho Yoo¹  Cheon Gyu Cho¹  Dae Hyuk Moon¹  Dong Jin Kim¹  Soo Jeong Lim¹  Seung Jun Oh¹ 

关键词: Alzheimer¡¯s disease;    A¥â42 fibrils;    Functionalized benzoxazoles;    Binding affinity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Functionalized benzoxazole derivatives were designed and synthesized based on the structural features of PIB and FDDNP, which show excellent binding affinities to aggregated A�?42 fibrils. All the synthesized compounds were evaluated by competitive binding assay against aggregated A�?42 fibrils using [125I]TZDM and displayed good in vitro binding affinities with Ki values (0.47-15.3 nM) from subnanomolar to nanomolar range. Among them, benzoxazoles 1f and 1a having malononitrile and ester moieties at C-6 exhibited superior binding affinities (K_i = 0.47 and 0.61 nM, respectively) to PIB (K_i = 0.77 nM).

【 授权许可】

Unknown