Here we describe the identification and preliminary characterization of a new class of pyrrolo(imidazo)quinoxaline hydrazones as flurescent probes for Aβ 1-42 fibrils. All the newly developed compounds were able to bind amyloid fibrils formed in vitro and some of them displayed an increase of their fluorescence upon binding. When tested on brain tissue preparations presenting Aβ deposits, the described hydrazones selectively stained amyloid structures and did not display aspecific binding. The hydrazones did not show antifibrillogenic activity and electron microscopy analysis revealed that they do not interfere with fibrils structure. The described pyrrolo(imidazo) quinoxalines could be useful for studying amyloid structures in vitro. Moreover, their experimentally proven ability to cross the blood-brain barrier in mouse opens the possibility of developing these compounds as potential amyloid imaging agents for in vivo applications.

Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils / Gemma, S.; Colombo, L.; Forloni, G.; Savini, L.; Fracasso, C.; Caccia, S.; Salmona, M.; Brindisi, M.; Yoshi, B. P.; Tripaldi, P.; Giorgi, G.; TAGLIALATELA SCAFATI, Orazio; Novellino, Ettore; Fiorini, I.; Campiani, G.; Butini, S.. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 9:(2011), pp. 5137-5148. [10.1039/c1ob05288h]

Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils

M. Brindisi;TAGLIALATELA SCAFATI, ORAZIO;NOVELLINO, ETTORE;
2011

Abstract

Here we describe the identification and preliminary characterization of a new class of pyrrolo(imidazo)quinoxaline hydrazones as flurescent probes for Aβ 1-42 fibrils. All the newly developed compounds were able to bind amyloid fibrils formed in vitro and some of them displayed an increase of their fluorescence upon binding. When tested on brain tissue preparations presenting Aβ deposits, the described hydrazones selectively stained amyloid structures and did not display aspecific binding. The hydrazones did not show antifibrillogenic activity and electron microscopy analysis revealed that they do not interfere with fibrils structure. The described pyrrolo(imidazo) quinoxalines could be useful for studying amyloid structures in vitro. Moreover, their experimentally proven ability to cross the blood-brain barrier in mouse opens the possibility of developing these compounds as potential amyloid imaging agents for in vivo applications.
2011
Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils / Gemma, S.; Colombo, L.; Forloni, G.; Savini, L.; Fracasso, C.; Caccia, S.; Salmona, M.; Brindisi, M.; Yoshi, B. P.; Tripaldi, P.; Giorgi, G.; TAGLIALATELA SCAFATI, Orazio; Novellino, Ettore; Fiorini, I.; Campiani, G.; Butini, S.. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 9:(2011), pp. 5137-5148. [10.1039/c1ob05288h]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/393949
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