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

Britt Marie Swahn*, David Wensbo, Johan Sandell, Daniel Sohn, Can Slivo, David Pyring, Jonas Malmström, Erwan Arzel, Michaela Vallin, Margareta Bergh, Fredrik Jeppsson, Allan E. Johnson, Anders Juréus, Jan Neelissen, Samuel Svensson

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    28 Scopus citations

    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 to PIB 1, as demonstrated by compounds 8 and 21.

    Original languageEnglish (US)
    Pages (from-to)1976-1980
    Number of pages5
    JournalBioorganic and Medicinal Chemistry Letters
    Volume20
    Issue number6
    DOIs
    StatePublished - Mar 15 2010

    Keywords

    • 2-Pyridylbenzofuran
    • 2-Pyridylbenzothiazole
    • 2-Pyridylbenzoxazole
    • Alzheimer
    • Carbon-11
    • Positron emission tomography, PET
    • β-Amyloid plaque

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

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