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Título: | Multitarget-Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases |
Autor: | Bautista-Aguilera, Óscar M. CSIC ORCID; Hagenow, S.; Palomino-Antolín, Alejandra; Farré-Alins, V.; Ismaili, L.; Joffrin, P. L.; Jimeno, M. Luisa CSIC ORCID; Soukup, Ondrej; Janockova, Jana; Kalinowski, A.; Proschak, E.; Iriepa, Isabel; Moraleda, I.; Schwed, J. S.; Romero Jódar, Alejandro CSIC ORCID; López-Muñoz, Francisco; Chioua, Mourad CSIC ORCID ; Egea, Javier; Ramsay, R. R.; Marco-Contelles, José CSIC ORCID; Stark, H. | Palabras clave: | Multitarget drugs Neurological agents Drug design Antioxidants Inhibitors |
Fecha de publicación: | 2017 | Editor: | John Wiley & Sons | Citación: | Angewandte Chemie International Edition 56: 12765-12769 (2017) | Resumen: | The therapy of complex neurodegenerative diseases requires the development of multitarget-directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards acetyl/butyrylcholinesterases and monoamine oxidases A/B as well as the histamine H receptor (H3R) were obtained by optimization of the neuroprotectant ASS234 by incorporating generally accepted H3R pharmacophore motifs. These small-molecule hits demonstrated balanced activities at the targets, mostly in the nanomolar concentration range. Additional in vitro studies showed antioxidative neuroprotective effects as well as the ability to penetrate the blood–brain barrier. With this promising in vitro profile, contilisant (at 1 mg kg i.p.) also significantly improved lipopolysaccharide-induced cognitive deficits. | Versión del editor: | http://dx.doi.org/10.1002/anie.201706072 | URI: | http://hdl.handle.net/10261/159113 | DOI: | 10.1002/anie.201706072 | Identificadores: | doi: 10.1002/anie.201706072 issn: 1433-7851 e-issn: 1521-3773 |
Aparece en las colecciones: | (IQOG) Artículos (CENQUIOR) Artículos |
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