Imaging Beta-Amyloid Peptides and Inhibition of Beta-Amyloid Peptide Aggregation

A method for treatment and/or prevention of beta-amyloid (Aβ) peptides aggregation-associated diseases by using carbazole-based fluorophores comprising a formula S series:

• said method comprising:
• binding said carbazole-based fluorophores to Aβ peptides, oligomers and/or fibrils thereof;
• inhibiting the growth and/or aggregation of said Aβ peptides, oligomers and/or fibrils upon said binding;
• and
• protecting neuronal cells against neurotoxic activities of the Aβ oligomers and/or fibrils;
• wherein Ar is a heteraromatic ring selected from the group consisting of pyridinyl, substituted pyridinyl, quinolinyl, substituted quinolinyl, acridinyl, substituted acridinyl, benzothiazolyl, substituted benzothiazolyl, benzoxazolyl, and substituted benzoxazolyl;
• R1 is a radical selected from the group consisting of polyethylene glycol chain, alkyl, substituted alkyl, peptide chain, glycosidyl, and C(O)NHCH((CH2CH2O)2CH3)2;
• R2 is selected from the group consisting of ethenyl, ethynyl, azo and azomethinyl.
• R3 is a radical selected from the group consisting of HO-alkyl, alkyl-COOalkyl, alkyl-CONH2, alkyl-CONHalkyl, polyethylene glycol chain;
• X is an anion selected from the group consisting of F, Cl, Br, I, HSO4, H2PO4, HCO3, tosylate, and mesylate;
• Y is selected from the group consisting of H, F, Cl, OH, and OCH3.