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

Int J Mol Sci

Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.

Published: January 2024

AI Article Synopsis

  • Progressive cognitive decline in Alzheimer's disease (AD) poses significant challenges, with current treatments offering only short-term relief through acetylcholinesterase inhibition.
  • Promising new approaches include butyrylcholinesterase inhibitors, multi-target ligands, and compounds targeting oxidative stress and inflammation, with cinnamate derivatives showing enhanced efficacy when combined with standard AD treatments.
  • Cinnamic acid stands out as a versatile structure with potential as an AD therapeutic, especially compounds with specific methoxy substitutions that improve effectiveness and suggest the need for further exploration of molecular size effects.

Article 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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10778916PMC
http://dx.doi.org/10.3390/ijms25010582DOI Listing

Publication Analysis

Top Keywords

cinnamic acid
12
alzheimer's disease
12
multi-target-directed cinnamic
4
acid hybrids
4
hybrids targeting
4
targeting alzheimer's
4
disease progressive
4
progressive cognitive
4
cognitive decline
4
decline alzheimer's
4

Similar Publications

Glucose is the most abundant monosaccharide and a principal substrate in biotechnological production processes. In Pseudomonas, this sugar is either imported directly into the cytosol or first oxidised to gluconate in the periplasm. While gluconate is taken up via a proton-driven symporter, the import of glucose is mediated by an ABC-type transporter, and hence both require energy.

View Article and Find Full Text PDF

New cinnamic acid sugar esters as potential UVB filters: Synthesis, cytotoxicity, and physicochemical properties.

Carbohydr Res

January 2025

Department of Biomolecular Sciences, University of Urbino "Carlo Bo", Campus Scientifico E. Mattei, via Ca' Le Suore 2, 61029, Urbino, PU, Italy. Electronic address:

Cinnamic Acid Sugar Ester Derivatives (CASEDs) are a class of natural compounds that exhibit several interesting biological activities. However, to date, no examples of their use in sunscreen formulations have been reported. Here, we describe the synthesis of a series of novel cinnamic acid esters of glucose (4a-g), ribose (4h) and lactose (4i) starting from the respective acetals 3.

View Article and Find Full Text PDF

Isoferulic acid (IA), a derivative of cinnamic acid, is derived from Danshen and exhibits anticancer properties by disrupting cancer cell activities. However, its role in pancreatic cancer, the "king of cancer", was unknown. In this study, pancreatic cancer cells were subjected to treatment with IA (6.

View Article and Find Full Text PDF

Colistin-resistant (COLR-Ab) is an opportunistic pathogen commonly associated with nosocomial infections, and it is difficult to treat with current antibiotics. Therefore, new antimicrobial agents need to be developed for treatment. Based on this information, we investigated the antimicrobial, antibiofilm, and combination activities of -coumaric acid (-CA), ferulic acid (FA), and -methoxycinnamic acid (-MCA) against five COLR-Ab isolates.

View Article and Find Full Text PDF

Cinnamic acid alleviates endothelial dysfunction and oxidative stress by targeting PPARδ in obesity and diabetes.

Chin Med

January 2025

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China.

Objective: Cinnamic acid (CA) is a bioactive compound isolated from cinnamon. It has been demonstrated to ameliorate inflammation and metabolic diseases, which are associated with endothelial dysfunction. This study was aimed to study the potential protective effects of CA against diabetes-associated endothelial dysfunction and its underlying mechanisms.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!