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Article

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)

Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari “Aldo Moro”, Via E. Orabona 4, 70125 Bari, Italy
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Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Cristobal De Los Rios and Raffaele Capasso
Molecules 2022, 27(3), 958; https://doi.org/10.3390/molecules27030958
Received: 17 December 2021 / Revised: 20 January 2022 / Accepted: 27 January 2022 / Published: 31 January 2022
(This article belongs to the Special Issue Small Molecules in Drug Discovery and Pharmacology)
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 Aβ 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. View Full-Text
Keywords: multi-target activity; PPAR agonists; enzymatic inhibition; Alzheimer’s disease multi-target activity; PPAR agonists; enzymatic inhibition; Alzheimer’s disease
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MDPI and ACS Style

Leuci, R.; Brunetti, L.; Laghezza, A.; Piemontese, L.; Carrieri, A.; Pisani, L.; Tortorella, P.; Catto, M.; Loiodice, F. 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 2022, 27, 958. https://doi.org/10.3390/molecules27030958

AMA Style

Leuci R, Brunetti L, Laghezza A, Piemontese L, Carrieri A, Pisani L, Tortorella P, Catto M, Loiodice F. 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. 2022; 27(3):958. https://doi.org/10.3390/molecules27030958

Chicago/Turabian Style

Leuci, Rosalba, Leonardo Brunetti, Antonio Laghezza, Luca Piemontese, Antonio Carrieri, Leonardo Pisani, Paolo Tortorella, Marco Catto, and Fulvio Loiodice. 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, no. 3: 958. https://doi.org/10.3390/molecules27030958

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