Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer's Disease.

Acetylcholinesterase / metabolism Alzheimer Disease / drug therapy Amyloid beta-Peptides Animals Butyrylcholinesterase / metabolism Cholinesterase Inhibitors / pharmacology Drug Design Mice Phenothiazines / pharmacology Structure-Activity Relationship Tacrine / pharmacology
Alzheimer’s disease acetylcholinesterase butyrylcholinesterase multitarget directed ligands phenothiazine tacrine

Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
05 05 2021
Historique:
pubmed: 15 4 2021
medline: 22 6 2021
entrez: 14 4 2021
Statut: ppublish

Résumé

Since 2002, no clinical candidate against Alzheimer's disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called "multitarget directed ligand" approach and designed 36 novel tacrine-phenothiazine heterodimers which were

Identifiants

DOI: 10.1021/acschemneuro.1c00184 PMID: 33852284
pubmed: 33852284
doi: 10.1021/acschemneuro.1c00184
doi:

Substances chimiques

Amyloid beta-Peptides 0
Cholinesterase Inhibitors 0
Phenothiazines 0
Tacrine 4VX7YNB537
Acetylcholinesterase EC 3.1.1.7
Butyrylcholinesterase EC 3.1.1.8

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1698-1715

Auteurs

Lukas Gorecki (L)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.
Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.
ORCID: 0000-0002-4791-6556

Elisa Uliassi (E)

Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.
ORCID: 0000-0002-0990-2532

Manuela Bartolini (M)

Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.
ORCID: 0000-0002-2890-3856

Jana Janockova (J)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.

Martina Hrabinova (M)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Vendula Hepnarova (V)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Lukas Prchal (L)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.

Lubica Muckova (L)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Jaroslav Pejchal (J)

Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Jana Z Karasova (JZ)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Eva Mezeiova (E)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.

Marketa Benkova (M)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.

Tereza Kobrlova (T)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.

Ondrej Soukup (O)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
ORCID: 0000-0001-6376-8701

Sabrina Petralla (S)

Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.

Barbara Monti (B)

Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.
ORCID: 0000-0003-0330-482X

Jan Korabecny (J)

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic.
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.
ORCID: 0000-0001-6977-7596

Maria Laura Bolognesi (ML)

Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6/Selmi 3, 40126 Bologna, Italy.
ORCID: 0000-0002-1289-5361

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Acetylcholinesterase › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Peptides bêta-amyloïdes › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Eucaryotes › Animaux › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Butyrylcholine esterase › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Anticholinestérasiques › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérocycliques 3 noyaux › Phénothiazines › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Phenothiazine-Tacrine Heterodimers: Pursuing...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérocycliques 3 noyaux › Acridines › Aminoacridines › Tacrine › Phenothiazine-Tacrine Heterodimers: Pursuing...