Alzheimer's Disease: An Update on Novel Therapeutics

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (20 June 2023) | Viewed by 1542

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1. LEPABE–Laboratory for Process Engineering, Environment, Biotechnology and Energy, R. Dr. Roberto Frias, 4200-465 Porto, Portugal
2. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: novel nanoengineered biomaterials for therapeutic applications; fluorinated peptide and active molecule interactions with surfaces and lipid model membranes; design of inhibitors of Alzheimer's fibrillogenesis; antibody-directed nanocarriers for Alzheimer’s disease; electrochemical immunosensors for detection of degenerative disease biomarkers; air pollutants/exposure risk assessment
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Guest Editor
1. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, R. Dr. Roberto Frias, 4200-465 Porto, Portugal
2. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: nanotechnology and interfacial phenomena; effects of fluorinated systems and peptides on the aggregation of amyloid beta peptides; conformational studies of protein and peptide self-organized systems and polymer surfaces; design and production of inorganic and polymeric nanosystems for pharmaceutical and food applications
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
2. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: drug delivery; targeted therapy; brain delivery; brain cancer; glioblastoma; cancer therapy; neurodegenerative disease therapy; biophysical models; drug–membrane interactions
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. ALiCE—Associate Laboratory in Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
2. LEPABE—Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal
Interests: nanotechnology; polymeric nanoparticles; lipid-based nanoparticles; drug delivery systems; targeted therapy; brain delivery; neurodegenerative disease therapy; effect of compounds on the aggregation and conformation of peptides and proteins; biophysical models; drug–membrane interactions; pharmaceutical and food applications
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Although some reversible treatments for Alzheimer's disease (AD) have been suggested recently, this debilitating condition is still incurable. The majority of clinically recommended treatments today only attenuate the symptoms, enhancing AD patients' quality of life. Despite their ability to attenuate symptoms, these medicines lead to several side effects. The absence of treatments for AD is due to a number of factors, including not knowing the real mechanism of the disease, even though several mechanisms have been proposed in the literature; the drugs being limited in reaching the brain due to the existence of the blood–brain barrier; and others.

Thus far, there is an urgent need to understand the disease mechanisms better and to develop novel treatments for AD. This Special Issue aims to collect the most recent advances in new treatments proposed for disease therapy.

Dr. Maria Carmo Pereira
Dr. Joana A. Loureiro
Dr. Maria João Ramalho
Dr. Stephanie Andrade
Guest Editors

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Keywords

  • blood–brain barrier
  • Alzheimer’s disease
  • neurological diseases
  • nanotechnology
  • novel treatments
  • dementia
  • drug targeting

Published Papers (1 paper)

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Research

29 pages, 10550 KiB  
Article
Anticholinesterase and Serotoninergic Evaluation of Benzimidazole–Carboxamides as Potential Multifunctional Agents for the Treatment of Alzheimer’s Disease
by Daria A. Belinskaia, Polina A. Voronina, Denis V. Krivorotov, Richard O. Jenkins and Nikolay V. Goncharov
Pharmaceutics 2023, 15(8), 2159; https://doi.org/10.3390/pharmaceutics15082159 - 19 Aug 2023
Cited by 2 | Viewed by 991
Abstract
The etiology and pathogenesis of Alzheimer’s disease are multifactorial, so one of the treatment strategies is the development of the drugs that affect several targets associated with the pathogenesis of the disease. Within this roadmap, we investigated the interaction of several substituted 1,3-dihydro-2-oxo-1 [...] Read more.
The etiology and pathogenesis of Alzheimer’s disease are multifactorial, so one of the treatment strategies is the development of the drugs that affect several targets associated with the pathogenesis of the disease. Within this roadmap, we investigated the interaction of several substituted 1,3-dihydro-2-oxo-1H-benzimidazol-2-ones with their potential molecular targets: cholinesterases (ChE) and three types of the Gs-protein-coupled serotonin receptors (5-HTR) 5-HT6, 5-HT4 and 5-HT7 (5-HT4R, 5-HT6R and 5-HT7R, respectively). A microplate modification of the Ellman method was used for the biochemical analysis of the inhibitory ability of the drugs towards ChE. Molecular modeling methods, such as molecular docking and molecular dynamics (MD) simulation in water and the lipid bilayer, were used to study the interaction of the compounds with ChE and 5-HTR. In vitro experiments showed that the tested compounds had moderate anticholinesterase activity. With the help of molecular modeling methods, the mechanism of interaction of the tested compounds with ChE was investigated, the binding sites were described and the structural features of the drugs that determine the strength of their anticholinesterase activity were revealed. Primary in silico evaluation showed that benzimidazole–carboxamides effectively bind to 5-HT4R and 5-HT7R. The pool of the obtained data allows us to choose N-[2-(diethylamino)ethyl]-2-oxo-3-(tert-butyl)-2,3-dihydro-1H-benzimidazole-1-carboxamide hydrochloride (compound 13) as the most promising for further experimental development. Full article
(This article belongs to the Special Issue Alzheimer's Disease: An Update on Novel Therapeutics)
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