Dual monoamine oxidase B and acetylcholine esterase inhibitors for treating movement and cognition deficits in a

6-hydroxydopamine multi-target phenotypic screen polypharmacy

Journal

Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents
ISSN: 1054-2523
Titre abrégé: Med Chem Res
Pays: United States
ID NLM: 9211347

Informations de publication

Date de publication:
May 2021
Historique:
entrez: 8 11 2021
pubmed: 9 11 2021
medline: 9 11 2021
Statut: ppublish

Résumé

Parkinson's disease (PD) is an age-associated neurodegenerative movement disorder that leads to loss of dopaminergic neurons and motor deficits. Approaches to neuroprotection and symptom management in PD include use of monoamine oxidase B (MAO-B) inhibitors. Many patients with PD also exhibit memory loss in the later stages of disease progression, which is treated with acetylcholine esterase (AChE) inhibitors. We sought to identify a dual-mechanism compound that would inhibit both MAO-B and AChE enzymes. Our screen identified a promising compound (7) with balanced MAO-B (IC

Identifiants

pubmed: 34744409
doi: 10.1007/s00044-021-02720-x
pmc: PMC8570587
mid: NIHMS1720470
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1166-1174

Subventions

Organisme : NIGMS NIH HHS
ID : P20 GM109098
Pays : United States
Organisme : NINDS NIH HHS
ID : R41 NS110070
Pays : United States
Organisme : NIA NIH HHS
ID : T32 AG052375
Pays : United States
Organisme : NIGMS NIH HHS
ID : U54 GM104942
Pays : United States

Déclaration de conflit d'intérêts

Conflict of Interest: The authors declare that they have no conflict of interest.

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Auteurs

Jacob Boos (J)

Department of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV, USA.
Department of Neuroscience, School of Medicine, West Virginia University, Morgantown, WV, USA.

Ahmed Shubbar (A)

Biomedical Sciences Program, Kent State University, Kent, OH, USA.

Werner J Geldenhuys (WJ)

Department of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV, USA.
Department of Neuroscience, School of Medicine, West Virginia University, Morgantown, WV, USA.

Classifications MeSH