Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
33984470
DOI
10.1016/j.bmcl.2021.128100
PII: S0960-894X(21)00326-7
Knihovny.cz E-resources
- Keywords
- Acetylcholinesterase, Alzheimer's disease, Amyloid-beta, Multi-target directed ligands, huprine Y, l-Tryptophan,
- MeSH
- Acetylcholinesterase metabolism MeSH
- Alzheimer Disease drug therapy metabolism MeSH
- Aminoquinolines chemistry pharmacology MeSH
- Amyloid beta-Peptides antagonists & inhibitors metabolism MeSH
- Cholinesterase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Heterocyclic Compounds, 4 or More Rings chemistry pharmacology MeSH
- Humans MeSH
- Molecular Structure MeSH
- Neuroprotective Agents chemical synthesis chemistry pharmacology MeSH
- Tryptophan chemistry pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Aminoquinolines MeSH
- Amyloid beta-Peptides MeSH
- Cholinesterase Inhibitors MeSH
- Heterocyclic Compounds, 4 or More Rings MeSH
- huprine Y MeSH Browser
- Neuroprotective Agents MeSH
- Tryptophan MeSH
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.
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