Tacrine is no longer used for the treatment of Alzheimer's disease (AD) as oral acetylcholinesterase (AChE) inhibitor (AChEI) mainly due to its hepatotoxic effects. Notwithstanding, it is still one of the most famous drugs. Indeed, since the discovery of the "non-cholinergic" AChE's activities and the seminal paper from Pang and coworkers reporting the discovery of a tacrine-dimer, bis(7)-tacrine, tacrine has been used from legions of medicinal chemists as a starting point to develop new multi target ligands (MTLs), able to interfere with biochemical pathways and targets whose dysregulation seems to be involved in the development of AD. This is the third review of a series concerning tacrine-based MTLs; in particular, in the present, we will summarize and discuss the most intriguing examples of tacrine-based MTLs published since 2013 until now.

Tacrine-based Multifunctional Agents in Alzheimer's Disease: an Old Story in Continuous Development

De Simone Angela;Tumiatti Vincenzo
2017-01-01

Abstract

Tacrine is no longer used for the treatment of Alzheimer's disease (AD) as oral acetylcholinesterase (AChE) inhibitor (AChEI) mainly due to its hepatotoxic effects. Notwithstanding, it is still one of the most famous drugs. Indeed, since the discovery of the "non-cholinergic" AChE's activities and the seminal paper from Pang and coworkers reporting the discovery of a tacrine-dimer, bis(7)-tacrine, tacrine has been used from legions of medicinal chemists as a starting point to develop new multi target ligands (MTLs), able to interfere with biochemical pathways and targets whose dysregulation seems to be involved in the development of AD. This is the third review of a series concerning tacrine-based MTLs; in particular, in the present, we will summarize and discuss the most intriguing examples of tacrine-based MTLs published since 2013 until now.
2017
24
999
1
1
Alzheimer`s Disease; Neurodegenerative diseases; acethylcholinesterase inhibitors.; dual binding acethylcholinesterase inhibitors; tacrine; tacrine hybrids
Milelli Andrea; De Simone Angela; Ticchi Nicole; Chen Huan Huan; Betari Nibal; Andrisano Vincenza; Tumiatti Vincenzo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1720221
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