Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
14 May 2020
Historique:
received: 27 12 2019
accepted: 07 02 2020
entrez: 22 5 2020
pubmed: 22 5 2020
medline: 22 5 2020
Statut: epublish

Résumé

Acetylcholinesterase (AChE) inhibitors (AChEIs) still remain the leading therapeutic options for the symptomatic treatment of cognitive deficits associated with mild-to-moderate Alzheimer's disease. The search for new AChEIs benefits from well-established knowledge of the molecular interactions of selective AChEIs, such as donepezil and related dual binding site inhibitors. Starting from a previously disclosed coumarin-based inhibitor (±)-

Identifiants

pubmed: 32435398
doi: 10.1021/acsmedchemlett.9b00656
pmc: PMC7236231
doi:

Types de publication

Journal Article

Langues

eng

Pagination

869-876

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Marco Catto (M)

Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Leonardo Pisani (L)

Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Eugenio de la Mora (E)

Univ. Grenoble Alpes, CEA, CNRS, Institute of Structural Biology, F-38044 Grenoble, France.

Benny Danilo Belviso (BD)

Institute of Crystallography, National Research Council (CNR), Via G. Amendola 122/O, 70126 Bari, Italy.

Giuseppe Felice Mangiatordi (GF)

Institute of Crystallography, National Research Council (CNR), Via G. Amendola 122/O, 70126 Bari, Italy.

Andrea Pinto (A)

Department of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, Via Celoria 2, 20133 Milano, Italy.

Annalisa De Palma (A)

Department of Biosciences, Biotechnologies and Biopharmaceutics, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Nunzio Denora (N)

Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Rocco Caliandro (R)

Institute of Crystallography, National Research Council (CNR), Via G. Amendola 122/O, 70126 Bari, Italy.

Jacques-Philippe Colletier (JP)

Univ. Grenoble Alpes, CEA, CNRS, Institute of Structural Biology, F-38044 Grenoble, France.

Israel Silman (I)

Department of Neurobiology, Weizmann Institute of Science, 7610001 Rehovot, Israel.

Orazio Nicolotti (O)

Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Cosimo Damiano Altomare (CD)

Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy.

Classifications MeSH