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Multi-target-directed ligands to combat neurodegenerative diseases.
The aims of the present article are to discuss the role of ligand modification in the discovery of clinically efficacious drugs and the role that ligands endowed with outstanding in vitro selectivity have in this area. Expand
Rational approach to discover multipotent anti-Alzheimer drugs.
Lipocrine is the first compound that inhibits the catalytic activity of A ChE and AChE-induced amyloid-beta aggregation and protects against reactive oxygen species and emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs. Expand
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
Compounds that inhibit acetylcholinesterase and NMDA receptor activity and display antioxidant properties are presented, emerging as lead candidates for treating AD. Expand
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
A new series of LA hybrids was designed and synthesized by combining racemic LA with motifs of other known anticholinesterase agents (rivastigmine and memoquin), which represents a step forward in the search for balanced anticholinergic and antioxidant capacities. Expand
A small molecule targeting the multifactorial nature of Alzheimer's disease.
Nowadays,Mechanism-based drug-design approaches are mainly directed toward two proteins, amy-loidb (Ab) and tau, whereas phosphorylated tau is the main component of neurofibrillary tangles, the other hallmark lesion of AD. Expand
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
A design strategy to convert a dual-binding site AChE inhibitor into triple functional compounds with promising in vitro profile against multifactorial syndromes, such as Alzheimer's disease, isExpand
A perspective on multi-target drug discovery and design for complex diseases
This Perspective will focus on the molecular and computational approaches that underpin drug design by medicinal chemists to promote understanding and collaboration with clinical scientists. Expand
Alzheimer's disease: new approaches to drug discovery.
The case study of the development of rasagiline provides an excellent example to support the validity of the multitarget-designed ligand approach to the search for effective medicines for combating Alzheimer's disease. Expand
Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.
The multifactorial mechanistic nature of cancer calls for the development of multifunctional therapeutic tools, i.e., single compounds able to interact with multiple altered pathogenetic pathways to induce apoptosis in tumor cell lines. Expand