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Synthesis of a Novel Series of Phosphonate-Functionalized 1,2,3-Triazoles as potential candidates for Allosteric Modulation of α7 Nicotinic Acetylcholine Receptors

1
Instituto de Química del Sur (INQUISUR-CONICET), Depto. de Química, Universidad Nacional del Sur, Av. Alem 1253, B8000CPB Bahía Blanca, Argentina
2
Depto. de Química, Universidad Nacional del Sur, Av. Alem 1253, B8000CPB Bahía Blanca, Argentina
*
Author to whom correspondence should be addressed.
Presented at the 22nd International Electronic Conference on Synthetic Organic Chemistry, 15 November- 15 December 2018; Available Online: https://sciforum.net/conference/ecsoc-22.
Proceedings 2019, 9(1), 35; https://doi.org/10.3390/ecsoc-22-05689
Published: 14 November 2018
PDF [346 KB, uploaded 1 April 2019]

Abstract

Nicotinic acetylcholine receptors (nAChR) are ligand-gated ion channels formed by the assembly of five subunits. Receptor activity could be subjected to both positive and negative modulation at allosteric sites by endogenous neurotransmitters as well as synthetic ligands such as steroids, bivalent cations, alcohols, and a range of drugs. The subtype of α7 nAChR has been considered a potential therapeutic target for Alzheimer’s disease, schizophrenia and other neurological and psychiatric disorders. In this work we present the synthesis of a novel series of phosphonate-functionalized 1,4-disubstituted 1,2,3-triazoles with potential activity over α7 AChR. These compounds were synthetized through the copper-catalyzed Huisgen 1,3-dipolar cycloaddition of organic azides and alkynes. Copper nanoparticles (CuNPs) immobilized on different supports were prepared using the CuCl2-Li-DTBB reducing system previously reported by our group.
Keywords: 1,2,3-triazoles; phosphonates; nicotinic receptors 1,2,3-triazoles; phosphonates; nicotinic receptors
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Stabile, S.A.; Vitale, C. Synthesis of a Novel Series of Phosphonate-Functionalized 1,2,3-Triazoles as potential candidates for Allosteric Modulation of α7 Nicotinic Acetylcholine Receptors. Proceedings 2019, 9, 35.

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