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Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils.
Gemma, Sandra; Colombo, Laura; Forloni, Gianluigi; Savini, Luisa; Fracasso, Claudia; Caccia, Silvio; Salmona, Mario; Brindisi, Margherita; Joshi, Bhupendra P; Tripaldi, Pierangela; Giorgi, Gianluca; Taglialatela-Scafati, Orazio; Novellino, Ettore; Fiorini, Isabella; Campiani, Giuseppe; Butini, Stefania.
Affiliation
  • Gemma S; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro, 53100, Siena, Italy.
Org Biomol Chem ; 9(14): 5137-48, 2011 Jul 21.
Article in En | MEDLINE | ID: mdl-21629961
Here we describe the identification and preliminary characterization of a new class of pyrrolo(imidazo)quinoxaline hydrazones as florescent probes for Aß(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 Aß 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.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Peptide Fragments / Quinoxalines / Amyloid beta-Peptides / Fluorescent Dyes / Hydrazones Limits: Animals Language: En Journal: Org Biomol Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article Affiliation country: Italy Country of publication: United kingdom

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Peptide Fragments / Quinoxalines / Amyloid beta-Peptides / Fluorescent Dyes / Hydrazones Limits: Animals Language: En Journal: Org Biomol Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article Affiliation country: Italy Country of publication: United kingdom