Acetylcholinesterase Inhibition of Diversely Functionalized Quinolinones for Alzheimer's Disease Therapy.

Acetylcholinesterase / metabolism Alzheimer Disease / drug therapy Cholinesterase Inhibitors / pharmacology Drug Design Drug Evaluation, Preclinical Humans Inhibitory Concentration 50 Kinetics Ligands Magnetic Resonance Spectroscopy Molecular Docking Simulation Monoamine Oxidase / metabolism Monoamine Oxidase Inhibitors / pharmacology Quinolones / pharmacology Recombinant Proteins / metabolism Structure-Activity Relationship
Alzheimer’s disease ChE/MAO inhibition contilisant dihydroquinolinones docking quinolinones synthesis

Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
30 May 2020
Historique:
received: 10 04 2020
revised: 14 05 2020
accepted: 26 05 2020
entrez: 4 6 2020
pubmed: 4 6 2020
medline: 31 3 2021
Statut: epublish

Résumé

In this communication, we report the synthesis and cholinesterase (ChE)/monoamine oxidase (MAO) inhibition of 19 quinolinones (

Identifiants

DOI: 10.3390/ijms21113913 PMID: 32486316 PMC: PMC7312762
pubmed: 32486316
pii: ijms21113913
doi: 10.3390/ijms21113913
pmc: PMC7312762
pii:
doi:

Substances chimiques

Cholinesterase Inhibitors 0
Ligands 0
Monoamine Oxidase Inhibitors 0
Quinolones 0
Recombinant Proteins 0
Monoamine Oxidase EC 1.4.3.4
monoamine oxidase A, human EC 1.4.3.4.
Acetylcholinesterase EC 3.1.1.7

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : MINECO
ID : SAF2015-65586-R
Organisme : UCJC
ID : UCJC 2020-03; UCJC 2020-33
Organisme : ERDF/ESF
ID : CZ.02.1.01/0.0/0.0/16_025/0007444
Organisme : University of Hradec Kralove
ID : SV2113-2019, VT2019-2021
Organisme : EU COST
ID : CA15135 MuTaLig

Références

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Auteurs

Óscar M Bautista-Aguilera (ÓM)

Department of Organic Chemistry and Inorganic Chemistry, Alcalá University, Alcalá de Henares, 28805 Madrid, Spain.
ORCID: 0000-0002-1327-1681

Lhassane Ismaili (L)

Laboratoire de Chimie Organique et Thérapeutique, Neurosciences Intégratives et Cliniques EA 481, University Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
ORCID: 0000-0002-6013-3150

Mourad Chioua (M)

Laboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006 Madrid, Spain.

Rudolf Andrys (R)

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.

Monika Schmidt (M)

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
ORCID: 0000-0003-4984-9155

Petr Bzonek (P)

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
ORCID: 0000-0001-9651-7917

María Ángeles Martínez-Grau (MÁ)

Lilly Research Laboratories, Eli Lilly & Company, Avda. de la Industria 30, Alcobendas, 28108 Madrid, Spain.

Christopher D Beadle (CD)

Lilly Research Centre, Eli Lilly & Company, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK.

Tatiana Vetman (T)

Lilly Research Laboratories, Eli Lilly & Company, Indianapolis, IN 46285, USA.

Francisco López-Muñoz (F)

Faculty of Health, Camilo José Cela University of Madrid (UCJC), 28692 Villafranca del Castillo, Spain.
Neuropsychopharmacology Unit, "Hospital 12 de Octubre" Research Institute, 28041 Madrid, Spain.
ORCID: 0000-0002-5188-6038

Isabel Iriepa (I)

Department of Organic Chemistry and Inorganic Chemistry, Alcalá University, Alcalá de Henares, 28805 Madrid, Spain.
Institute of Chemical Research Andrés M. del Río, Alcalá University, Alcalá de Henares, 28805 Madrid, Spain.

Bernard Refouvelet (B)

Laboratoire de Chimie Organique et Thérapeutique, Neurosciences Intégratives et Cliniques EA 481, University Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.

Kamil Musilek (K)

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03 Hradec Kralove, Czech Republic.
ORCID: 0000-0002-7504-4062

José Marco-Contelles (J)

Laboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006 Madrid, Spain.

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Acetylcholinesterase › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Anticholinestérasiques › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Concentration inhibitrice 50 › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Analyse spectrale › Spectroscopie par résonance magnétique › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH2 group donors › Monoamine oxidase › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de la monoamine oxydase › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinoléines › Quinolinone › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines recombinantes › Acetylcholinesterase Inhibition of Diversely...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Acetylcholinesterase Inhibition of Diversely...