Imaging beta-amyloid peptides and inhibition of beta-amyloid peptide aggregation

摘要

The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro by using carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using carbazole-based fluorophores.

主权项

1. A method of labeling, imaging and detecting beta-amyloid (Aβ) peptides, oligomers and fibrils by administering carbazole-based fluorophores comprising a formula S or V series:to
a subject being labeled imaged or detected for Aβ peptides, oligomers and fibrils, wherein Ar is a heteraromatic ring selected from the group consisting of pyridinyl, substituted pyridinyl, quinolinyl, substituted qunoiinyl, acridinyl, substituted acridinyl, benzothiazolyl, substituted benzothiazolyl, henzoxazolyl, and substituted benzoxazolyl; R1 is 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 selected from the group consisting of alkyl, HO-alkyl, HS-alkyl, H2N-alkyl, HN-alkyl-alkyl, HOOC-alkyl, (alkyl)3N+-alkyl, and (Ph)3P+-alkyl; and X is an anion selected from the group consisting of F−, Cl−, Br−, I−, HSO4−, H2PO4−, HCO3−, tosylate, and mesylate.