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Communication

Triazolopyridopyrimidine: A New Scaffold for Dual-Target Small Molecules for Alzheimer’s Disease Therapy

1
Laboratory of Applied Chemistry: Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax. B. P 802. 3000 Sfax, Tunisia
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Laboratoire de Chimie Organique et Thérapeutique, Neurosciences intégratives et cliniques EA 481, University Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France
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Department of Organic Chemistry and Inorganic Chemistry, School Sciences, University of Alcalá, Ctra. Barcelona, Km. 33.6, 28871 Alcalá de Henares, Spain
4
Laboratory of Medicinal Chemistry (IQOG, CSIC) C/Juan de la Cierva 3, 28006 Madrid, Spain
*
Authors to whom correspondence should be addressed.
Academic Editor: Paula Sério Branco
Molecules 2020, 25(14), 3190; https://doi.org/10.3390/molecules25143190
Received: 22 June 2020 / Revised: 9 July 2020 / Accepted: 12 July 2020 / Published: 13 July 2020
(This article belongs to the Special Issue Development of New Methods of Synthesis of Heterocycles)
Alzheimer’s disease (AD) is multifactorial disease characterized by the accumulation of abnormal extracellular deposits of amyloid-beta (Aβ) peptide, and intracellular neurofibrillary tangles (NFTs), along with dramatic neuronal death and decreased levels of choline acetyltransferase. Given the limited therapeutic success of available drugs, it is urgent to explore all the opportunities available to combat this illness. Among them, the discovery of new heterocyclic scaffolds binding different receptors involved in AD should offer structural diversity and new therapeutic solutions. In this context, this work describes new triazolopyridopyrimidine easily prepared in good yields showing anticholinesterase inhibition and strong antioxidant power, particularly the most balanced: 6-amino-5-(4-methoxyphenyl)-2-phenyl-[1,2,4]triazolo[1′,5′:1,6] pyrido[2,3-d]pyrimidine-4-carbonitrile(3c) with IC50 equal to 1.32 μM against AChE and oxygen radical absorbance capacity (ORAC) value equal to 4.01 Trolox equivalents (TE); thus representing a new and very promising hit-triazolopyridopyrimidine for AD therapy. View Full-Text
Keywords: antioxidants; cholinesterase inhibitors; ORAC; triazolopyridopyrimidine antioxidants; cholinesterase inhibitors; ORAC; triazolopyridopyrimidine
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MDPI and ACS Style

Zribi, L.; Pachòn-Angona, I.; Bautista-Aguilera, Ò.M.; Diez-Iriepa, D.; Marco-Contelles, J.; Ismaili, L.; Iriepa, I.; Chabchoub, F. Triazolopyridopyrimidine: A New Scaffold for Dual-Target Small Molecules for Alzheimer’s Disease Therapy. Molecules 2020, 25, 3190. https://doi.org/10.3390/molecules25143190

AMA Style

Zribi L, Pachòn-Angona I, Bautista-Aguilera ÒM, Diez-Iriepa D, Marco-Contelles J, Ismaili L, Iriepa I, Chabchoub F. Triazolopyridopyrimidine: A New Scaffold for Dual-Target Small Molecules for Alzheimer’s Disease Therapy. Molecules. 2020; 25(14):3190. https://doi.org/10.3390/molecules25143190

Chicago/Turabian Style

Zribi, Lazhar, Irene Pachòn-Angona, Òscar M. Bautista-Aguilera, Daniel Diez-Iriepa, José Marco-Contelles, Lhassane Ismaili, Isabel Iriepa, and Fakher Chabchoub. 2020. "Triazolopyridopyrimidine: A New Scaffold for Dual-Target Small Molecules for Alzheimer’s Disease Therapy" Molecules 25, no. 14: 3190. https://doi.org/10.3390/molecules25143190

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