Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer's Disease

Progressive cognitive decline in Alzheimer's disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only temporary relief. Promising alternatives include butyrylcholinesterase (BuChE) inhibitors, multi-target ligands (MTDLs) that address th...

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Published inInternational journal of molecular sciences Vol. 25; no. 1; p. 582
Main Authors Drakontaeidi, Aliki, Pontiki, Eleni
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 01.01.2024
MDPI
Subjects
acetylcholinesterase inhibition
Advertising executives
Alzheimer's disease
Amino acids
antioxidant
Antioxidants
Brain research
Cell cycle
cinnamic acids
Cognition & reasoning
Development and progression
Disease
Drugs
Enzyme kinetics
Health aspects
hybrids
Inflammation
Medical research
multi-target
Oxidative stress
Pathophysiology
Patient compliance
Proteins
Review
Target marketing
antioxidant
Alzheimer’s disease
neuroprotective
acetylcholinesterase inhibition
cinnamic acids
hybrids
multi-target
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Abstract Progressive cognitive decline in Alzheimer's disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only temporary relief. Promising alternatives include butyrylcholinesterase (BuChE) inhibitors, multi-target ligands (MTDLs) that address the multi-factorial nature of AD, and compounds that target oxidative stress and inflammation. Cinnamate derivatives, known for their neuroprotective properties, show potential when combined with established AD agents, demonstrating improved efficacy. They are being positioned as potential AD therapeutic leads due to their ability to inhibit Aβ accumulation and provide neuroprotection. This article highlights the remarkable potential of cinnamic acid as a basic structure that is easily adaptable and combinable to different active groups in the struggle against Alzheimer's disease. Compounds with a methoxy substitution at the para-position of cinnamic acid display increased efficacy, whereas electron-withdrawing groups are generally more effective. The effect of the molecular volume is worthy of further investigation.
AbstractList Progressive cognitive decline in Alzheimer’s disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only temporary relief. Promising alternatives include butyrylcholinesterase (BuChE) inhibitors, multi-target ligands (MTDLs) that address the multi-factorial nature of AD, and compounds that target oxidative stress and inflammation. Cinnamate derivatives, known for their neuroprotective properties, show potential when combined with established AD agents, demonstrating improved efficacy. They are being positioned as potential AD therapeutic leads due to their ability to inhibit Aβ accumulation and provide neuroprotection. This article highlights the remarkable potential of cinnamic acid as a basic structure that is easily adaptable and combinable to different active groups in the struggle against Alzheimer’s disease. Compounds with a methoxy substitution at the para-position of cinnamic acid display increased efficacy, whereas electron-withdrawing groups are generally more effective. The effect of the molecular volume is worthy of further investigation.
Audience Academic
Author Pontiki, Eleni
Drakontaeidi, Aliki
AuthorAffiliation Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; alikdrak@pharm.auth.gr
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  givenname: Aliki
  surname: Drakontaeidi
  fullname: Drakontaeidi, Aliki
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  givenname: Eleni
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  surname: Pontiki
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  organization: Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
BackLink https://www.ncbi.nlm.nih.gov/pubmed/38203753$$D View this record in MEDLINE/PubMed
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Keywords antioxidant
Alzheimer’s disease
neuroprotective
acetylcholinesterase inhibition
cinnamic acids
hybrids
multi-target
Language English
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Snippet Progressive cognitive decline in Alzheimer's disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only...
Progressive cognitive decline in Alzheimer’s disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only...
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SubjectTerms acetylcholinesterase inhibition
Advertising executives
Alzheimer's disease
Amino acids
antioxidant
Antioxidants
Brain research
Cell cycle
cinnamic acids
Cognition & reasoning
Development and progression
Disease
Drugs
Enzyme kinetics
Health aspects
hybrids
Inflammation
Medical research
multi-target
Oxidative stress
Pathophysiology
Patient compliance
Proteins
Review
Target marketing
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Title Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer's Disease
URI https://www.ncbi.nlm.nih.gov/pubmed/38203753
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Volume 25
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