4.5 Article

Proflavine derivatives as fluorescent imaging agents of amyloid deposits

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 8, Pages 2203-2206

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.010

Keywords

Proflavine; Click chemistry; Fluorescent markers; Amyloid deposits imaging

Funding

  1. NIA NIH HHS [R01 AG021982] Funding Source: Medline

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A series of proflavine derivatives for use to further image A beta amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23 months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on A beta(40) fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new A beta imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections. (C) 2011 Elsevier Ltd. All rights reserved.

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