Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto, Japan.
Bioorg Med Chem. 2011 Jul 1;19(13):4148-53. doi: 10.1016/j.bmc.2011.04.049. Epub 2011 May 3.
A series of benzofuran-2-yl(phenyl)methanone derivatives were synthesized and evaluated as novel probes for β-amyloid plaques. These derivatives were produced by a Rap-Stoermer condensation reaction. Compounds with a N,N-dimethylamino group displayed high affinity for Aβ(1-42) aggregates with K(i) values in the nanomolar range. Autoradiography with brain sections of AD model mice (APP/PS1) revealed that a radioiodinated probe, [(125)I]10, labeled β-amyloid plaques selectively and displayed good brain uptake (3.53% ID/g) at 2 min. The results suggest that benzofuran-2-yl(phenyl)methanone derivatives should be investigated further as potential probes for detecting β-amyloid plaques in the AD brain.
一系列苯并呋喃-2-基（苯基）甲酮衍生物被合成并评估为新型β-淀粉样斑块探针。这些衍生物是通过 Rap-Stoermer 缩合反应产生的。具有 N,N-二甲基氨基的化合物对 Aβ（1-42）聚集体具有高亲和力，K（i）值在纳摩尔范围内。用 AD 模型小鼠（APP/PS1）的脑切片进行放射自显影显示，放射性碘标记探针 [(125)I]10 选择性标记β-淀粉样斑块，并在 2 分钟时显示出良好的脑摄取（3.53% ID/g）。结果表明，苯并呋喃-2-基（苯基）甲酮衍生物应作为探测 AD 脑中β-淀粉样斑块的潜在探针进一步研究。
