Výsledky vyhledávání - "Rocío Lajarín-Cuesta"

In Silico Prediction of the Toxic Potential of Neuroprotective Bifunctional Molecules Based on Chiral N-Propargyl-1,2-amino Alcohol Derivatives

Autor: Eva Ramos, Raquel L Arribas, Javier Egea, Cristóbal de los Ríos, Laura González-Lafuente, Eva M. García-Frutos, Rocío Lajarín-Cuesta, Alejandro Romero

Publikováno v: E-Prints Complutense. Archivo Institucional de la UCM
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Chemical Research in Toxicology

N-Propargylamines are useful synthetic scaffolds for the synthesis of bioactive molecules, and in addition, they possess important pharmacological activities. We obtained several neuroprotective molecules, chiral 1,2-amino alcohols and 1,2-diamines,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f3b71afe9ed768944ba0bd5d2cfdf81
https://eprints.ucm.es/id/eprint/69284/1/acs.chemrestox.0c00519.pdf

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Design and synthesis of multipotent 3-aminomethylindoles and 7-azaindoles with enhanced protein phosphatase 2A-activating profile and neuroprotection

Autor: Eva M. García-Frutos, Carmen Nanclares, Raquel L Arribas, Luis Gandía, Cristóbal de los Ríos, Rocío Lajarín-Cuesta

Publikováno v: European Journal of Medicinal Chemistry. 157:294-309

We report the synthesis and pharmacological evaluation of new 3-aminomethylindoles derivatives with neuroprotective properties designed to present multi-target activity centered on reducing the neuronal Ca2+ overload and preventing phosphatase 2A (PP

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::186db91f78cc584139e16633afd823c6
https://doi.org/10.1016/j.ejmech.2018.07.030

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Substituent effect of N-benzylated gramine derivatives that prevent the PP2A inhibition and dissipate the neuronal Ca2+ overload, as a multitarget strategy for the treatment of Alzheimer’s disease

Autor: Dorleta Gonzalez, Lucía Viejo, Cristóbal de los Ríos, Rocío Lajarín-Cuesta, Raquel L Arribas

Publikováno v: Bioorganic & Medicinal Chemistry. 26:2551-2560

Following the premises of the multitarget-directed ligands approach for the drug RD nevertheless that substitution provoked loss of viability at 100-fold higher concentrations (10 μM), what discards them for a deeper pharmacological study. Overall,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::06044f81eb15e4301ca15b0f46c17c47
https://doi.org/10.1016/j.bmc.2018.04.019

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Ligands for Ser/Thr phosphoprotein phosphatases: a patent review (2005-2015)

Autor: Cristóbal de los Ríos, Rocío Lajarín-Cuesta, Raquel L Arribas

Publikováno v: Expert Opinion on Therapeutic Patents. 26:389-407

The role played by phosphoprotein phosphatases (PPP) enzymes makes them of interest as therapeutic targets to treat pathologies including neurodegenerative diseases, cancer and autoimmune diseases, but also liable to cause severe side effects. This f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ae2c78bc5c1cf2f07d43ff5dad7d577
https://doi.org/10.1517/13543776.2016.1135903

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Benzothiazepine CGP37157 and its 2′-isopropyl analogue modulate Ca2+ entry through CALHM1

Autor: Rocío Lajarín-Cuesta, Francisco J. Martínez-Sanz, Cristóbal de los Ríos, María F. Cano-Abad, Ana J. Moreno-Ortega

Publikováno v: Neuropharmacology. 95:503-510

CALHM1 is a Ca(2+) channel discovered in 2008, which plays a key role in the neuronal electrical activity, among other functions. However, there are no known efficient blockers able to modulate its Ca(2+) handling ability. We herein describe that ben

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::14731caefa28f6d00a80f2ae2c3d63ab
https://doi.org/10.1016/j.neuropharm.2015.02.016

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Optimization of Bicyclic Lactam Derivatives as NMDA Receptor Antagonists

Autor: María Isabel Rodríguez-Franco, Margarida Espadinha, Lídia Gonçalves, Cristóbal de los Ríos, Clara Herrera-Arozamena, Rocío Lajarín-Cuesta, Jorge Dourado, Maria M. M. Santos

Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
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N-Methyl-d-aspartate (NMDA) receptors are fundamental for the normal function of the central nervous system (CNS), and play an important role in memory and learning. Over-activation of these receptors leads to neuronal loss associated with major neur

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b3fb434dfbc6eeb9212106bf5835939
http://hdl.handle.net/10261/149788

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PP2A Ligand ITH12246 Protects against Memory Impairment and Focal Cerebral Ischemia in Mice

Autor: Mercedes Villarroya, Laura González-Lafuente, Francisco J. Martínez-Sanz, Martín Estrada, Abdelouahid Samadi, Cristóbal de los Ríos, María Isabel Rodríguez-Franco, José Marco-Contelles, Rocío Lajarín-Cuesta, Alejandro Romero, Silvia Lorrio, Manuela G. López

Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
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ITH12246 (ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8] naphthyridine-3-carboxylate) is a 1,8-naphthyridine described to feature an interesting neuroprotective profile in in vitro models of Alzheimer's disease. These effects were proposed to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ca2e954f75cb49b94b7784eeb4d957e
https://doi.org/10.1021/cn400050p

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Gramine derivatives targeting Ca2+ channels and Ser/Thr phosphatases: A new dual strategy for the treatment of neurodegenerative diseases

Autor: Cristóbal de los Ríos, Laura González-Lafuente, Luis Gandía, Rocío Lajarín-Cuesta, Juan Alberto Arranz-Tagarro, Carmen Nanclares, Monique Araújo de Brito, Raquel A. Arribas

Publikováno v: Biblos-e Archivo. Repositorio Institucional de la UAM
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This document is the unedited author's version of a Submitted Work that was subsequently accepted for publication in Journal of Medicinal Chemistry , copyright © American Chemical Society after peer review. To access the final edited and published w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00013949be21dcf8489fbdcb5f7c95f1
http://hdl.handle.net/10486/676459

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