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

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

The syntheses and SAR of new series of b-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 a...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1976-1980
Hauptverfasser: 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
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Sprache:eng
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Zusammenfassung:The syntheses and SAR of new series of b-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. AB:
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.01.105