Synthesis and evaluation of pyridylbenzofuran, pyridylbenzothiazole and pyridylbenzoxazole derivatives as 18 F-PET imaging agents for β-amyloid plaques

…, A Juréus, J Neelissen, P Johnström, M Schou…

文献索引：Swahn, Britt-Marie; Sandell, Johan; Pyring, David; Bergh, Margareta; Jeppsson, Fredrik; Jureus, Anders; Neelissen, Jan; Johnstroem, Peter; Schou, Magnus; Svensson, Samuel Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 13 p. 4332 - 4337

全文：HTML全文

被引用次数: 19

摘要

The synthesis and SAR of new β-amyloid binding agents are reported. Evaluation of important properties for achieving good signal-to-background ratio is described. Compounds 27, 33, and 36 displayed desirable lipophilic and pharmacokinetic properties. Compound 27 was further evaluated with autoradiographic studies in vitro on human brain tissue and in vivo in Tg2576 mice. Compound 27 showed an increased signal-to- ...