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Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain.

Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Research Abstract Details 

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  • Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Abstract Text:

    masahiro onoMasahiro Ono,miyuki horiMiyuki Hori,mamoru haratakeMamoru Haratake,takami tomiyamaTakami Tomiyama,hiroshi moriHiroshi Mori,morio nakayamaMorio Nakayama,

    A series of novel chalcones and their related derivatives were synthesized and evaluated as beta-amyloid imaging probes. In the structure-activity relationship of binding affinities to synthetic Abeta(1-42) aggregates, compound 14 displayed the highest binding affinity in vitro. beta-Amyloid plaques in the Alzheimer's model mouse brain were visualized with 14. In biodistribution studies using normal mice, [(125)I]14 showed good brain uptake (2.56% ID/g, 2min postinjection) and rapid washout from the brain (0.21% ID/g, 60min postinjection). These results suggest that [(125)I]14 should be further investigated as a potentially useful beta-amyloid imaging probe.

    Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Publishing Authors By Initials

    m onoM Ono,m horiM Hori,m haratakeM Haratake,t tomiyamaT Tomiyama,h moriH Mori,m nakayamaM Nakayama,

    For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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    Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Journal Published:

    PUBLICATION TYPE: Research Support, Non-U.S. Gov

    Journal: Bioorganic & medicinal chemistry

    VOLUME: 15

    Page Numbers: 6388-96

    Journal Abbreviation: Bioorg. Med. Chem.

    ISSN: 0968-0896

    DAY: 4

    MONTH: 07

    YEAR: 2007

    Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Information

    Number of References:

    LANGUAGE: eng

    NlmUniqueID: 9413298

    Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Keywords Mesh Terms:

    KEYWORDS: Structure-Activity Relationship

    MESH TERMS: metabolism

    Chemical & Substance for Abstract: Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain. Information

    Substance Name: Ligands

    Registry Number: 0

    Grant and Affiliation Information for Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain.

    AFFILIATION: Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan. mono@nagasaki-u.ac.jp

    Country: England

    England Research PublicationEngland Research Publication

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    MEDLINETA: Bioorg Med Chem

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