Title:From Antioxidant Chelators to Site-Activated Multi-Target Chelators Targeting Hypoxia Inducing Factor, Beta-Amyloid, Acetylcholinesterase and Monoamine Oxidase A/B
VOLUME: 12 ISSUE: 5
Author(s):H. Zheng, M. Fridkin and M. B.H. Youdim
Affiliation:Department of Medicinal Chemistry, Intra-cellular Therapies Inc. 3960 Broadway, New York, NY 10032, USA.
Keywords:AChE-MAO A/B inhibitors, HLA20, HLA20A, M30, M30D, multi-target chelators, site-activated, Alzheimer’s
disease
Abstract:chelators hold great promise as disease-modifying drugs for Alzheimer’s therapy, and recent research efforts
have focused on designing multi-target chelators with increased targeting and efficacy through rational drug design. In
this review, we discuss our research studies on the rational design of new multi-target chelators with the potential not only
to simultaneously modulate several disease-related targets, but also contain features designed to improve the BBB
permeability, increase the brain targeting, and minimize potential side effects. These new chelators include
neuroprotective chelators with brain selective monoamine oxidase (MAO) A/B inhibitory activity, acetylcholinesterase
(AChE) inhibitors with site-activated chelating and neurogenesis activity, and AChE-MAO A/B inhibitors with siteactivated
chelating and neurogenesis activity.
