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Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jul 01; Vol. 43, pp. 128100. Date of Electronic Publication: 2021 May 10. - Publication Year :
- 2021
-
Abstract
- The search for novel and effective therapeutics for Alzheimer's disease (AD) is the main quest that remains to be resolved. The goal is to find a disease-modifying agent able to confront the multifactorial nature of the disease positively. Herewith, a family of huprineY-tryptophan heterodimers was prepared, resulting in inhibition of cholinesterase and neuronal nitric oxide synthase enzymes, with effect against amyloid-beta (Aβ) and potential ability to cross the blood-brain barrier. Their cholinesterase pattern of behavior was inspected using kinetic analysis in tandem with docking studies. These heterodimers exhibited a promising pharmacological profile with strong implication in AD.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Alzheimer Disease metabolism
Aminoquinolines chemistry
Amyloid beta-Peptides antagonists & inhibitors
Amyloid beta-Peptides metabolism
Cholinesterase Inhibitors chemical synthesis
Cholinesterase Inhibitors chemistry
Dose-Response Relationship, Drug
Heterocyclic Compounds, 4 or More Rings chemistry
Humans
Molecular Structure
Neuroprotective Agents chemical synthesis
Neuroprotective Agents chemistry
Structure-Activity Relationship
Tryptophan chemistry
Acetylcholinesterase metabolism
Alzheimer Disease drug therapy
Aminoquinolines pharmacology
Cholinesterase Inhibitors pharmacology
Heterocyclic Compounds, 4 or More Rings pharmacology
Neuroprotective Agents pharmacology
Tryptophan pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 43
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 33984470
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.128100