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

Abstract

The syntheses and SAR of new series of beta-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 to PIB 1, as demonstrated by compounds 8 and 21.

DOI: 10.1016/j.bmcl.2010.01.105

Cite this paper

@article{Swahn2010SynthesisAE, title={Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11C-PET imaging agents for beta-amyloid plaques.}, author={Britt-Marie Swahn and David Wensbo and Johan Sandell and Daniel Sohn and Can Slivo and David Pyring and Jonas Malmstr{\"{o}m and Erwan Arzel and Michaela Vallin and Margareta Bergh and Fredrik Jeppsson and Allan E Johnson and Anders Jur{\'e}us and Jan Neelissen and Samuel Svensson}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 6}, pages={1976-80} }