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Molecules 2018, 23(1), 230; https://doi.org/10.3390/molecules23010230

Towards a Novel Class of Multitarget-Directed Ligands: Dual P2X7–NMDA Receptor Antagonists

1
Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia i Ciències de l’Alimentació, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Joan XXIII 27–31, E-08028 Barcelona, Spain
2
School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Cheomdangwagi-ro, Buk-gu, 123, Gwangju 61005, Korea
3
Unitat de Farmacologia, Facultat de Medicina i Ciències de la Salut, Universitat Rovira i Virgili, c./St. Llorenç 21, E-43201 Reus, Spain
*
Authors to whom correspondence should be addressed.
Received: 2 December 2017 / Revised: 15 January 2018 / Accepted: 16 January 2018 / Published: 21 January 2018
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Abstract

Multi-target-directed ligands (MTDLs) offer new hope for the treatment of multifactorial complex diseases such as Alzheimer’s Disease (AD). Herein, we present compounds aimed at targeting the NMDA and the P2X7 receptors, which embody a different approach to AD therapy. On one hand, we are seeking to delay neurodegeneration targeting the glutamatergic NMDA receptors; on the other hand, we also aim to reduce neuroinflammation, targeting P2X7 receptors. Although the NMDA receptor is a widely recognized therapeutic target in treating AD, the P2X7 receptor remains largely unexplored for this purpose; therefore, the dual inhibitor presented herein—which is open to further optimization—represents the first member of a new class of MTDLs. View Full-Text
Keywords: Alzheimer’s disease; dual target compounds; neuroinflammation; NMDA; P2X7 Alzheimer’s disease; dual target compounds; neuroinflammation; NMDA; P2X7
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Karoutzou, O.; Kwak, S.-H.; Lee, S.-D.; Martínez-Falguera, D.; Sureda, F.X.; Vázquez, S.; Kim, Y.-C.; Barniol-Xicota, M. Towards a Novel Class of Multitarget-Directed Ligands: Dual P2X7–NMDA Receptor Antagonists. Molecules 2018, 23, 230.

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