Leuci_2022_Molecules_27_

Reference

Title : A New Series of Aryloxyacetic Acids Endowed with Multi-Target Activity towards Peroxisome Proliferator-Activated Receptors (PPARs), Fatty Acid Amide Hydrolase (FAAH), and Acetylcholinesterase (AChE) - Leuci_2022_Molecules_27_
Author(s) : Leuci R , Brunetti L , Laghezza A , Piemontese L , Carrieri A , Pisani L , Tortorella P , Catto M , Loiodice F
Ref : Molecules , 27 : , 2022
Abstract :

A new series of aryloxyacetic acids was prepared and tested as peroxisome proliferator-activated receptors (PPARs) agonists and fatty acid amide hydrolase (FAAH) inhibitors. Some compounds exhibited an interesting dual activity that has been recently proposed as a new potential therapeutic strategy for the treatment of Alzheimer's disease (AD). AD is a multifactorial pathology, hence multi-target agents are currently one of the main lines of research for the therapy and prevention of this disease. Given that cholinesterases represent one of the most common targets of recent research, we decided to also evaluate the effects of our compounds on the inhibition of these specific enzymes. Interestingly, two of these compounds, (S)-5 and 6, showed moderate activity against acetylcholinesterase (AChE) and even some activity, although at high concentration, against Abeta peptide aggregation, thus demonstrating, in agreement with the preliminary dockings carried out on the different targets, the feasibility of a simultaneous multi-target activity towards PPARs, FAAH, and AChE. As far as we know, these are the first examples of molecules endowed with this pharmacological profile that might represent a promising line of research for the identification of novel candidates for the treatment of AD.

PubMedSearch : Leuci_2022_Molecules_27_
PubMedID: 35164223

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Citations formats

Leuci R, Brunetti L, Laghezza A, Piemontese L, Carrieri A, Pisani L, Tortorella P, Catto M, Loiodice F (2022)
A New Series of Aryloxyacetic Acids Endowed with Multi-Target Activity towards Peroxisome Proliferator-Activated Receptors (PPARs), Fatty Acid Amide Hydrolase (FAAH), and Acetylcholinesterase (AChE)
Molecules 27 :

Leuci R, Brunetti L, Laghezza A, Piemontese L, Carrieri A, Pisani L, Tortorella P, Catto M, Loiodice F (2022)
Molecules 27 :