Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines.

Alzheimer Disease / drug therapy Animals Drug Discovery / methods Humans Tacrine / chemistry
Alzheimer's disease Cholinesterases Multi-target-directed ligands Neuroprotection PyridoTacrines Tacrine

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
15 Mar 2019
Historique:
received: 18 12 2018
revised: 25 01 2019
accepted: 02 02 2019
pubmed: 12 2 2019
medline: 27 3 2019
entrez: 12 2 2019
Statut: ppublish

Résumé

Tacrine was the first drug approved for the treatment of Alzheimer's disease (AD) in 1993, which was withdrawn in 2013 due to its hepatotoxicity. However, new, non-hepatotoxic tacrine derivatives have been constantly searched for. In this context, since 1997, we have prepared a number of diversely functionalized tacrines by changing the benzene ring present in tacrine to five- or six-membered aromatic ring cores that could present anticholinesterasic activity and additional pharmacological properties. The new compounds were designed as juxtaposed structures between tacrine and the well-known Ca

Identifiants

DOI: 10.1016/j.ejmech.2019.02.005 PMID: 30739821
pubmed: 30739821
pii: S0223-5234(19)30115-1
doi: 10.1016/j.ejmech.2019.02.005
pii:
doi:

Substances chimiques

Tacrine 4VX7YNB537

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

381-389

Informations de copyright

Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Auteurs

Cristóbal de Los Ríos (C)

Instituto de Investigación Sanitaria, Servicio de Farmacología Clínica, Hospital Universitario de la Princesa, 28006, Madrid, Spain; Instituto de I + D del Medicamento Teófilo Hernando (ITH), Facultad de Medicina, Universidad Autónoma de Madrid, 28029, Madrid, Spain. Electronic address: cristobal.delosrios@inv.uam.es.

José Marco-Contelles (J)

Laboratory of Medicinal Chemistry (IQOG, CSIC), 3, Juan de la Cierva, 28006, Madrid, Spain. Electronic address: iqoc21@iqog.csic.es.

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Classifications MeSH

questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Tacrines for Alzheimer's disease therapy. III....
questionsmedicales.fr › Eucaryotes › Animaux › Tacrines for Alzheimer's disease therapy. III....
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Tacrines for Alzheimer's disease therapy. III....
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Tacrines for Alzheimer's disease therapy. III....
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérocycliques 3 noyaux › Acridines › Aminoacridines › Tacrine › Tacrines for Alzheimer's disease therapy. III....