Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease

…, FJ Luque, M Medina, A Martínez

Index: Castro, Ana; Hernandez, Laura; Dorronsoro, Isabel; Saenz, Patricia; Perez, Concepcion; Kalko, Susana; Orozco, Modesto; Luque, F. Javier; Martinez, Ana Medicinal Chemistry Research, 2002 , vol. 11, # 4 p. 219 - 237

Full Text: HTML

Citation Number: 140

Abstract

New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as new potent drugs that may simultaneously alleviate cognitive deficits and behave as disease-modifying agents by inhibiting the β-amyloid (Aβ) peptide aggregation through binding to both catalytic and peripheral sites of the enzyme. Particularly, compounds 5 and 6 emerged as the most potent heterodimers reported so far, displaying IC50 values ...