A review. To date, the pharmacotherapy of Alzheimer's disease (AD) has been based on acetylcholinesterase inhibitors (AChEIs), and more recently on an N-methyl-D-aspartate receptor antagonist. By increasing acetylcholine concn. in the brain, AChEIs slow behavioral and functional impairments, improving cognitive function. The review provides an update on novel analogs of approved AChEIs, their combination with other anti-AD agents, natural AChEIs, and modern multitarget-directed ligands (MTDLs) able to hit different biol. targets. The authors reviewed patents filed during 2005-2007 dealing with new AChEIs and their potential application for AD treatment. The authors point out new chem. structures and scaffolds for designing new AD therapeutic agents as well as new combinations or MTDLs. Compared to the limited no. of novel com. available AChEI analogs, many new natural compds. were patented for AD treatment. These might represent a starting point for the rational design of new MTDLs.

Progress in acetylcholinesterase inhibitors for Alzheimer's disease: an update

TUMIATTI, VINCENZO;BOLOGNESI, MARIA LAURA;MINARINI, ANNA;ROSINI, MICHELA;MILELLI, ANDREA;MATERA, RICCARDO;MELCHIORRE, CARLO
2008

Abstract

A review. To date, the pharmacotherapy of Alzheimer's disease (AD) has been based on acetylcholinesterase inhibitors (AChEIs), and more recently on an N-methyl-D-aspartate receptor antagonist. By increasing acetylcholine concn. in the brain, AChEIs slow behavioral and functional impairments, improving cognitive function. The review provides an update on novel analogs of approved AChEIs, their combination with other anti-AD agents, natural AChEIs, and modern multitarget-directed ligands (MTDLs) able to hit different biol. targets. The authors reviewed patents filed during 2005-2007 dealing with new AChEIs and their potential application for AD treatment. The authors point out new chem. structures and scaffolds for designing new AD therapeutic agents as well as new combinations or MTDLs. Compared to the limited no. of novel com. available AChEI analogs, many new natural compds. were patented for AD treatment. These might represent a starting point for the rational design of new MTDLs.
V. Tumiatti; M. L. Bolognesi; A. Minarini; M. Rosini; A. Milelli; R. Matera; C. Melchiorre
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/66192
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