Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders

Abstract

Neurodegenerative diseases represent a challenge for biomedical research due to their high prevalence and lack of mechanism-based treatments. Because of the complex pathology of neurodegenerative disorders, multifunctional drugs have been increasingly recognized as potential treatments. We identified homobivalent γ-carbolinium salts as potent inihitors of both cholinesterases, <i>N</i>-methyl-d-aspartate receptors, and monoamine oxidases. Homobivalent γ-carbolines displayed similar structure–activity relationships on all tested targets and may present promising designed multiple ligands for the treatment of neurodegenerative disorders