2-Phenylbenzothiazolyl iridium complexes as inhibitors and probes of amyloid β aggregation

Karna Terpstra, Yiran Huang, Hanah Na, Liang Sun, Citlali Gutierrez, Zhengxin Yu, Liviu M. Mirica

Research output: Contribution to journalArticlepeer-review

Abstract

The aggregation of amyloid β (Aβ) peptides is a significant hallmark of Alzheimer's disease (AD), and the detection of Aβ aggregates and the inhibition of their formation are important for the diagnosis and treatment of AD, respectively. Herein, we report a series of benzothiazole-based Ir(iii) complexes HN-1 to HN-8 that exhibit appreciable inhibition of Aβ aggregation in vitro and in living cells. These Ir(iii) complexes can induce a significant fluorescence increase when binding to Aβ fibrils and Aβ oligomers, while their measured log D values suggest these compounds could have enhanced blood-brain barrier (BBB) permeability. In vivo studies show that HN-1, HN-2, HN-3, and HN-8 successfully penetrate the BBB and stain the amyloid plaques in AD mouse brains after a 10-day treatment, suggesting that these Ir(iii) complexes could act as lead compounds for AD therapeutic and diagnostic agent development.

Original languageEnglish (US)
Pages (from-to)14258-14264
Number of pages7
JournalDalton Transactions
Volume53
Issue number34
DOIs
StatePublished - Aug 6 2024

ASJC Scopus subject areas

  • Inorganic Chemistry

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