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  • Title: Novel quinoxaline derivatives for in vivo imaging of β-amyloid plaques in the brain.
    Author: Cui M, Ono M, Kimura H, Liu B, Saji H.
    Journal: Bioorg Med Chem Lett; 2011 Jul 15; 21(14):4193-6. PubMed ID: 21684159.
    Abstract:
    In a search for new probes to detect β-amyloid plaques in the brain of patients with Alzheimer's disease (AD), we have synthesized and evaluated a series of quinoxaline derivatives containing a '6+6-6' ring system. These quinoxaline derivatives showed excellent affinity for Aβ(1-42) aggregates with K(i) values ranging from 2.6 to 10.7nM. Autoradiography with sections of brain tissue from an animal model of AD mice (APP/PS1) and AD patients revealed that [(125)I]5 labeled β-amyloid plaques specifically. In biodistribution experiments using normal mice, [(125)I]5 displayed high uptake (6.03% ID/g at 2min) into and a moderately fast washout from the brain. Although additional refinements are needed to decrease the lipophilicity and improve the washout rate, the quinoxaline scaffold may be useful as a backbone structure to develop novel β-amyloid imaging agents.
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