Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.

Acetylcholinesterase / metabolism Alzheimer Disease / drug therapy Animals Cholinesterase Inhibitors / chemistry Cholinesterases Donepezil / therapeutic use Lead / therapeutic use Ligands Zebrafish / metabolism

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
22 09 2022
Historique:
pubmed: 10 9 2022
medline: 24 9 2022
entrez: 9 9 2022
Statut: ppublish

Résumé

Drug development efforts that focused on single targets failed to provide effective treatment for Alzheimer's disease (AD). Therefore, we designed cholinesterase inhibition (ChEI)-based multi-target-directed ligands (MTDLs) to simultaneously target AD-related receptors. We built a library of 70 compounds, sequentially screened for ChEI, and determined σ

Identifiants

DOI: 10.1021/acs.jmedchem.2c01003 PMID: 36084304
pubmed: 36084304
doi: 10.1021/acs.jmedchem.2c01003
doi:

Substances chimiques

Cholinesterase Inhibitors 0
Ligands 0
Lead 2P299V784P
Donepezil 8SSC91326P
Acetylcholinesterase EC 3.1.1.7
Cholinesterases EC 3.1.1.8

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

12292-12318

Commentaires et corrections

Type : ErratumIn

Auteurs

Bengisu Turgutalp (B)

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.
German Centre for Neurodegenerative Diseases (DZNE), Helmholtz Association, 01307 Dresden, Germany.
ORCID: 0000-0001-8507-5420

Prabesh Bhattarai (P)

German Centre for Neurodegenerative Diseases (DZNE), Helmholtz Association, 01307 Dresden, Germany.
Department of Neurology, Columbia University Irving Medical Center, 10032 New York, United States.

Tugba Ercetin (T)

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, TRNC, via Mersin 10, 99628 Famagusta, Turkey.

Chiara Luise (C)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-Universität Halle-Wittenberg, 6099 Halle (Saale), Germany.

Rengin Reis (R)

Department of Toxicology, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.
Department of Toxicology, Faculty of Pharmacy, Acibadem Mehmet Ali Aydinlar University, 34758 Istanbul, Turkey.

Enise Ece Gurdal (EE)

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.
Institute of Chemistry, Martin-Luther-Universität Halle-Wittenberg, 06120 Halle, Germany.
ORCID: 0000-0003-1064-8639

Andreas Isaak (A)

European Institute for Molecular Imaging (EIMI), der Westfälischen Wilhelms-Universität, D-48149 Münster, Germany.

Derya Biriken (D)

German Centre for Neurodegenerative Diseases (DZNE), Helmholtz Association, 01307 Dresden, Germany.
Department of Medical Microbiology, Ankara University Faculty of Medicine, 06620 Ankara, Turkey.

Elisabeth Dinter (E)

German Centre for Neurodegenerative Diseases (DZNE), Helmholtz Association, 01307 Dresden, Germany.
Department of Neurology, University Clinic, TU Dresden, 01307 Dresden, Germany.

Hande Sipahi (H)

Department of Toxicology, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.

Dirk Schepmann (D)

Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, D-48149 Münster, Germany.

Anna Junker (A)

European Institute for Molecular Imaging (EIMI), der Westfälischen Wilhelms-Universität, D-48149 Münster, Germany.

Bernhard Wünsch (B)

Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, D-48149 Münster, Germany.
ORCID: 0000-0002-9030-8417

Wolfgang Sippl (W)

Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-Universität Halle-Wittenberg, 6099 Halle (Saale), Germany.
ORCID: 0000-0002-5985-9261

Hayrettin Ozan Gulcan (HO)

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, TRNC, via Mersin 10, 99628 Famagusta, Turkey.

Caghan Kizil (C)

German Centre for Neurodegenerative Diseases (DZNE), Helmholtz Association, 01307 Dresden, Germany.
Department of Neurology, Columbia University Irving Medical Center, 10032 New York, United States.

Mine Yarim (M)

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Acetylcholinesterase › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Anticholinestérasiques › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Composés polycycliques › Hydrocarbures aromatiques polycycliques › Indènes › Indanes › Donépézil › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Produits chimiques inorganiques › Métaux › Métaux lourds › Plomb › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Discovery of Potent Cholinesterase...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Poissons › Cypriniformes › Cyprinidae › Danio zébré › Discovery of Potent Cholinesterase...