TY - JOUR
T1 - Proflavine derivatives as fluorescent imaging agents of amyloid deposits
AU - Garin, Dominique
AU - Oukhatar, Fatima
AU - Mahon, Andrew B.
AU - Try, Andrew C.
AU - Dubois-Dauphin, Michel
AU - Laferla, Frank M.
AU - Demeunynck, Martine
AU - Sallanon, Marcelle Moulin
AU - Chierici, Sabine
PY - 2011/4/15
Y1 - 2011/4/15
N2 - A series of proflavine derivatives for use to further image Aβ 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 Aβ40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.
AB - A series of proflavine derivatives for use to further image Aβ 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 Aβ40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.
KW - proflavine
KW - click chemistry
KW - fluorescent markers
KW - amyloid deposits imaging
UR - http://www.scopus.com/inward/record.url?scp=79953290815&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2011.03.010
DO - 10.1016/j.bmcl.2011.03.010
M3 - Article
C2 - 21435875
AN - SCOPUS:79953290815
SN - 0960-894X
VL - 21
SP - 2203
EP - 2206
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 8
ER -