Design, synthesis, and evaluation of novel bifunctional iron-chelators as potential agents for neuroprotection in Alzheimer's, Parkinson's, and other neurodegenerative diseases

Hailin Zheng, Lev M. Weiner, Orit Bar-Am, Silvina Epsztejn, Z. Ioav Cabantchik, Abraham Warshawsky, Moussa B.H. Youdim, Mati Fridkin

Research output: Contribution to journalArticlepeer-review

278 Scopus citations

Abstract

Several novel antioxidant-iron chelators bearing 8-hydroxyoxyquinoline moiety were synthesized, and various properties related to their iron chelation, and neuroprotective action were investigated. All the chelators exhibited strong iron(III) chelating and high antioxidant properties. Chelator 9 (HLA20), having good permeability into K562 cells and moderate selective MAO-B inhibitory activity (IC 50 110 μM), displayed the hightest protective effects against differentiated P19 cell death induced by 6-hydroxydopamine. EPR studies suggested that Chelator 9 also act as radical scavenger to directly scavenge hydroxyl radical.

Original languageEnglish
Pages (from-to)773-783
Number of pages11
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number3
DOIs
StatePublished - 1 Feb 2005

Keywords

  • 8-Hydroxyquinoline
  • Antioxidant-iron chelator
  • Lipid peroxidation
  • Neuroprotection

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