Synthetic strategies and medicinal chemistry perspectives of dual acting carbonic anhydrase modulators with monoamine oxidase and cholinesterase inhibitors

RSC Medicinal Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Янв. 1, 2025

Dual acting carbonic anhydrase modulators with monoamine oxidase and cholinesterase inhibitors.

Язык: Английский

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Therapeutic Role of Heterocyclic Compounds in Neurodegenerative Diseases: Insights from Alzheimer’s and Parkinson’s Diseases

Neurology International, Год журнала: 2025, Номер 17(2), С. 26 - 26

Опубликована: Фев. 7, 2025

Alzheimer’s and Parkinson’s are the most common neurodegenerative diseases (NDDs). The development of aberrant protein aggregates progressive permanent loss neurons major characteristic features these disorders. Although precise mechanisms causing disease (AD) (PD) still unknown, there is a wealth evidence suggesting that misfolded proteins, accumulation dysfunction neuroreceptors mitochondria, dysregulation enzymes, release neurotransmitters significantly influence pathophysiology diseases. There no effective protective medicine or therapy available even with availability numerous medications. an urgent need to create new powerful bioactive compounds since number people NDDs rising globally. Heterocyclic have consistently played pivotal role in drug discovery due their exceptional pharmaceutical properties. Many clinically approved drugs, such as galantamine hydrobromide, donepezil hydrochloride, memantine opicapone, feature heterocyclic cores. As therapeutic potential, heterocycles intriguing research topic for drugs PD AD. This review aims provide current insights into potential use targeting diverse targets manage potentially treat patients AD PD.

Язык: Английский

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Chemical composition, antioxidant activities, and enzyme inhibitory effects of Lespedeza bicolour Turcz. essential oil

Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2025, Номер 40(1)

Опубликована: Фев. 6, 2025

Lespedeza bicolour Turcz. is a traditional medicinal plant with wide range of ethnomedicinal values. The main components L. essential oil (EO) were β-pinene (15.41%), β-phellandrene (12.43%), and caryophyllene (7.79%). EO showed antioxidant activity against ABTS radical DPPH an IC50 value 0.69 ± 0.03 mg/mL 10.44 2.09 mg/mL, respectively. FRAP was 81.96 6.17 μmol/g. had activities acetylcholinesterase, α-glucosidase, β-lactamase values 309.30 11.16 μg/mL, 360.47 35.67 27.54 1.21 Molecular docking methyl dehydroabietate docked well all tested enzymes. Sclareol (+)-borneol acetate the strongest binding affinity to α-glucosidase β-lactamase, present study provides direction for searching enzyme inhibitors three enzymes shows possesses potential treat series diseases.

Язык: Английский

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Synthesis and Characterization of Thiazole Derivatives as Cholinesterase Inhibitors

ChemistrySelect, Год журнала: 2025, Номер 10(11)

Опубликована: Март 1, 2025

Abstract Fifteen new thiazole derivatives were synthesized and their cholinesterase inhibitory activities evaluated. The design of these compounds involves linking rings to a cyclopropyl moiety, followed by substitutions with various amine groups. structures the thiazole‐cyclopropyl confirmed using IR, HRMS, ¹H‐NMR, ¹ 3 C‐NMR, HPLC, single‐crystal X‐ray diffraction. Compounds 6g 6h found crystallize in monoclinic system space group P21/c , featuring α γ angles 90°. Cholinesterase inhibition was assessed Ellman method. While most exhibited weak effects on butyrylcholinesterase (BuChE), they showed significant acetylcholinesterase (AChE). Compound 6l potent AChE activity, an IC₅₀ 0.079 ± 0.16 µM, comparable Donepezil (IC₅₀ = 0.056 0.22 µM). Molecular docking, molecular dynamics simulations, MM/GBSA binding free energy calculations stable interactions between compound peripheral anionic site AChE. Furthermore, metal ion chelation studies demonstrated that as multitarget‐directed ligand, effectively chelated biologically relevant ions. In summary, shows potential inhibitor represents promising lead for further research development Alzheimer's disease treatment.

Язык: Английский

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Application of magnetic aldehyde-functionalized ionic liquids for immobilization of acetylcholinesterase

International Journal of Biological Macromolecules, Год журнала: 2025, Номер unknown, С. 143101 - 143101

Опубликована: Апрель 1, 2025

Язык: Английский

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Tripeptides inhibit dual targets AChE and BACE-1: a computational study

RSC Advances, Год журнала: 2025, Номер 15(16), С. 12866 - 12875

Опубликована: Янв. 1, 2025

Computational identification of tripeptides as promising dual AChE/BACE-1 inhibitors for Alzheimer's therapy.

Язык: Английский

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Novel Dual Acetyl- and Butyrylcholinesterase Inhibitors Based on the Pyridyl–Pyridazine Moiety for the Potential Treatment of Alzheimer’s Disease

Pharmaceuticals, Год журнала: 2024, Номер 17(10), С. 1407 - 1407

Опубликована: Окт. 21, 2024

: Alzheimer's disease (AD) is characterized by cholinergic dysfunction, making the inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) critical for improving neurotransmission. However, development effective dual inhibitors remains challenging.

Язык: Английский

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