Synthesis and evaluation of thioflavin-T analogs as potential imaging agents for amyloid plaques
作者:Soon Jae Jung、Yong Dae Park、Jeong Hoon Park、Seung Dae Yang、Min Goo Hur、Kook Hyun Yu
DOI:10.1007/s00044-012-0414-2
日期:2013.9
AbstractThioflavin-T (ThT) is a benzothiazole dye that exhibits enhanced fluorescence upon binding to beta-amyloid (Aβ) plaques and is commonly used in the diagnosis of Alzheimer’s disease (AD). In this study, the ThT analogs were designed and synthesized, and screening was conducted for the detection of Aβ 40 fibrils in vitro. Among these compounds, 2-(2′-methoxy-4′-methylaminophenyl)benzoxazole (2) meets two critical
摘要硫磺素T(ThT的)是一种苯并噻唑染料,其表现出增强的荧光在结合至β-淀粉状蛋白(A β)斑块和阿尔茨海默氏病(AD)的诊断是常用的。在这项研究中,的ThT类似物设计并合成,以及筛选用于检测的进行β 40个体外原纤维。在这些化合物中,2-(2'-甲氧基-4'-甲基氨基苯基)苯并恶唑(2)满足显像剂的两个关键要求:与ThT相比,其更高的荧光响应性和更强的结合亲和力。该化合物显示出最高的结合亲和力与3.27±0.29μM的解离常数,并且选择性地染色的β聚集在SHSY5Y神经母细胞瘤细胞中。这一发现证明了该化合物作为AD研究的脑成像剂的潜在用途。 图形概要