Conjugates of amiridine and salicylic derivatives as promising multifunctional CNS agents for potential treatment of Alzheimer's disease DOI Creative Commons
Галина Ф. Махаева, Maria V. Grishchenko, N. V. Kovaleva

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 358(1)

Published: Dec. 17, 2024

New conjugates of amiridine and salicylic derivatives (salicylamide, salicylimine, salicylamine) with different lengths alkylene spacers were designed, synthesized, evaluated as potential multifunctional central nervous system therapeutic agents for Alzheimer's disease (AD). Conjugates demonstrated high acetylcholinesterase (AChE) butyrylcholinesterase (BChE) inhibition (IC

Language: Английский

Synthesis of conjugates of ipidacrine with oxa/azaheterocycles and their potential as agents for the treatment of Alzheimer’s disease DOI
О. Г. Худина, Maria V. Grishchenko, Галина Ф. Махаева

et al.

Russian Chemical Bulletin, Journal Year: 2024, Volume and Issue: 73(6), P. 1755 - 1765

Published: June 1, 2024

Language: Английский

Citations

1
Polyfluorinated benzoic acids as promising reagents for organic synthesis and medicinal chemistry DOI
Evgeny V. Shchegolkov, Yanina V. Burgart,

Irina V. Shchur

et al.

Russian Chemical Reviews, Journal Year: 2024, Volume and Issue: 93(8), P. RCR5131 - RCR5131

Published: Aug. 1, 2024

Polyfluoroaromatic compounds occupy a special place in organic synthesis due to wide range of their chemical transformations and unique biological properties. The introduction the carboxyl function into polyfluoroarenes allows further diversification chemistry these compounds. This review summarizes data on polyfluorobenzoic acids, including derivatives polyfluorosalicylic acids. reactions esterification, amidation, reduction, decarboxylation, metal-catalyzed decarboxylative cross-coupling, C–H functionalization, reductive defluorination, nucleophilic aromatic substitution, heterocyclization complex formation are considered. Reactivity features polyfluorobenzoates comparison non-fluorinated counterparts highlighted. potential for practical applications acid derivatives, primarily as biologically active compounds, is presented. <br> Bibliography includes 300 references.

Language: Английский

Citations

1
Therapeutic Options in Alzheimer’s Disease: From Classic Acetylcholinesterase Inhibitors to Multi-Target Drugs with Pleiotropic Activity DOI Creative Commons
Ramón Cacabelos,

Olaia Martínez-Iglesias,

Natalia Cacabelos

et al.

Life, Journal Year: 2024, Volume and Issue: 14(12), P. 1555 - 1555

Published: Nov. 26, 2024

Alzheimer’s disease (AD) is a complex/multifactorial brain disorder involving hundreds of defective genes, epigenetic aberrations, cerebrovascular alterations, and environmental risk factors. The onset the neurodegenerative process triggered decades before first symptoms appear, probably due to combination genomic phenomena. Therefore, primary objective any effective treatment intercept in its presymptomatic phases. Since approval acetylcholinesterase inhibitors (Tacrine, Donepezil, Rivastigmine, Galantamine) Memantine, between 1993 2003, no new drug was approved by FDA until advent immunotherapy with Aducanumab 2021 Lecanemab 2023. Over past decade, more than 10,000 compounds potential action on some pathogenic components AD have been tested. limitations these anti-AD treatments stimulated search for multi-target (MT) drugs. In recent years, 1000 drugs MT function studied models. aim address complex multifactorial nature disease. This approach has offer comprehensive benefits single-target therapies, which may be limited their effectiveness intricate pathology AD. A strategy still unexplored agents. Another option could biotechnological products pleiotropic action, among nosustrophine-like represent an attractive, although not definitive, example.

Language: Английский

Citations

1
Recent Advancements in the Treatment of Alzheimer’s Disease: A Multitarget-directed Ligand Approach DOI
Sumit Kumar, Amol T. Mahajan,

Ramesh Ambatwar

et al.

Current Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 31(37), P. 6032 - 6062

Published: Dec. 27, 2023

: Alzheimer's disease (AD) is a neurodegenerative and one of the leading causes progressive dementia, affecting 50 million people worldwide. Many pathogenic processes, including amyloid β aggregation, tau hyperphosphorylation, oxidative stress, neuronal death, deterioration function cholinergic neurons, are associated with its progression. The one-compound-one-target treatment paradigm was unsuccessful in treating AD due to multifaceted nature disease. recent develop-ment multitarget-directed ligand research has been explored target complemen-tary pathways We aimed find key role progress MTDLs AD; thus, we searched for past ten years literature on “Pub-Med”, “ScienceDirect”, “ACS” “Bentham Science” using keywords neurodegen-erative diseases, Alzheimer’s disease, ligands. further filtered based quality work relevance AD. Thus, this review high-lights current advancement advantages ligands over tradi-tional single-targeted drugs their development treat

Language: Английский

Citations

2
Conjugates of tacrine with aminomethylidene derivatives of ethyl acetoacetate as promising agents for the treatment of Alzheimer’s disease DOI
Maria V. Grishchenko, Галина Ф. Махаева,

Ya.V. Burgart

et al.

Russian Chemical Bulletin, Journal Year: 2023, Volume and Issue: 72(12), P. 2994 - 3004

Published: Dec. 1, 2023

Language: Английский

Citations

1
Meet the Section Editor DOI
С. О. Бачурин

Current Neuropharmacology, Journal Year: 2024, Volume and Issue: 22(10), P. 1577 - 1577

Published: April 26, 2024

Language: Английский

Citations

0
Design, Synthesis and Biological Evaluation of New Thiosemicarbazone-Acridine Derivatives as Multi-Target-Directed Ligand (Mtdl) for Alzheimer's Disease DOI
Gleyton Leonel Silva Sousa, Nathália Fonseca Nadur, Larissa A. Ferreira

et al.

Published: Jan. 1, 2024

Language: Английский

Citations

0
2-Arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropanoic acids as selective and effective carboxylesterase inhibitors with powerful antioxidant potential DOI
Yanina V. Burgart, Галина Ф. Махаева, О. Г. Худина

et al.

Bioorganic & Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 115, P. 117938 - 117938

Published: Oct. 3, 2024

Language: Английский

Citations

0
Discovery of novel thiosemicarbazone-acridine targeting butyrylcholinesterase with antioxidant, metal complexing and neuroprotector abilities as potential treatment of Alzheimer's disease: in vitro, in vivo, and in silico studies. DOI
Gleyton Leonel Silva Sousa, Nathália Fonseca Nadur, Larissa A. Ferreira

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 281, P. 117030 - 117030

Published: Nov. 7, 2024

Language: Английский

Citations

0
A Novel Galantamine–Curcumin Hybrid Inhibits Butyrylcholinesterase: A Molecular Dynamics Study DOI Creative Commons

Evdokiya Salamanova,

Mariyana Atanasova, Irini Doytchinova

et al.

Chemistry, Journal Year: 2024, Volume and Issue: 6(6), P. 1645 - 1657

Published: Dec. 16, 2024

Cholinesterases are enzymes that break down the neurotransmitter acetylcholine in nervous system. The two main types acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). AChE inhibitors used to treat Alzheimer’s disease by increasing levels. BChE activity increases later stages of Alzheimer’s, suggesting it might contribute disease. In previous experiments, was found a newly designed hybrid galantamine (GAL) curcumin (CCN) (compound 4b) decreases murine brain homogenates. Here, we explore this observation using molecular dynamics simulations. GAL CCN were also studied for comparison. structures complexes between ligands predicted docking. Then, simulations performed evaluate stability interactions enzyme over simulated time 1 μs. All three formed stable with BChE. Compound 4b more hydrogen bonds other compared CCN, stronger binding affinity. explain its superior anti-BChE observed experiments.

Language: Английский

Citations

0