Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11 C-PET imaging agents for β-amyloid plaques

…, M Bergh, F Jeppsson, AE Johnson, A Juréus…

Index: Swahn, Britt-Marie; Wensbo, David; Sandell, Johan; Sohn, Daniel; Slivo, Can; Pyring, David; Malmstroem, Jonas; Arzel, Erwan; Vallin, Michaela; Bergh, Margareta; Jeppsson, Fredrik; Johnson, Allan E.; Jureus, Anders; Neelissen, Jan; Svensson, Samuel Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 6 p. 1976 - 1980

Full Text: HTML

Citation Number: 24

Abstract

The syntheses and SAR of new series of β-amyloid binding agents are reported. The effort to optimize signal-to-background ratios for these ligands are described. Compounds 8, 21 and 30 displayed desirable lipophilicity and pharmacokinetic properties. Compounds 8 and 21 were evaluated with in vitro autoradiographic studies and in vivo in APP/PS1 transgenic mice. It is shown that it was possible to increase the signal-to-background ratios compared ...