[3 + 2] Cycloaddition Synthesis of New (Chromene‐1,3,4‐Oxadiazole) Hybrids Linked to Pyrazole Units as Potential Acetylcholinesterase Inhibitors

ChemistrySelect, Год журнала: 2025, Номер 10(2)

Опубликована: Янв. 1, 2025

Abstract A lot of interest has been gained recently in developing novel acetylcholinesterase (AChE) inhibitors that can alleviate Alzheimer's symptoms. In the current study, we aimed to explore AChE inhibitory activity new chromenes attached 1,3,4‐oxadiazole and/or pyrazole units. The hybrids were obtained via [3 + 2] cycloaddition reaction between appropriate chromene‐based enaminones and hydrazonyl chlorides. inhibition percentages products against recorded at tested concentrations 15 25 µM compared donepezil. 3‐(3‐Acetyl‐1‐(4‐methoxyphenyl)‐1 H ‐pyrazole‐4‐carbonyl)‐6‐(((5‐phenyl‐1,3,4‐oxadiazol‐2‐yl)thio)methyl)‐2 ‐chromen‐2‐one displayed promising with 73.2 87.3, respectively, aforementioned concentrations. Moreover, previous hybrid gave 2,2‐diphenylpicrylhydrazyl (DPPH) using reference ascorbic acid. It had an percentage 86.6 a concentration µM.

Язык: Английский

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Exploring Fluorine-Substituted Piperidines as Potential Therapeutics for Diabetes Mellitus and Alzheimer’s Diseases

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 273, С. 116523 - 116523

Опубликована: Май 21, 2024

Язык: Английский

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Development of multifunctional fluorescence-emitting potential theranostic agents for Alzheimer’s disease

Talanta, Год журнала: 2025, Номер 287, С. 127574 - 127574

Опубликована: Янв. 11, 2025

Язык: Английский

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Innovative approaches to Alzheimer's therapy: Harnessing the power of heterocycles, oxidative stress management, and nanomaterial drug delivery system

Ageing Research Reviews, Год журнала: 2024, Номер 97, С. 102298 - 102298

Опубликована: Апрель 10, 2024

Язык: Английский

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Recent advancements in the synthesis of fused thienopyridines and their therapeutic applications

European Journal of Medicinal Chemistry Reports, Год журнала: 2024, Номер 12, С. 100185 - 100185

Опубликована: Июль 2, 2024

Fused thienopyridines represent a class of heterocyclic molecules that have garnered increasing attention due to their unique structural features and versatile chemical properties. This review systematically examines the latest synthetic methodologies employed in preparing fused thienopyridine derivatives, emphasizing innovative approaches contribute diversity. Moreover, discussion extends broad spectrum therapeutic applications offer, encompassing utility different diseases. The explores pharmacological activities biological properties thienopyridines, shedding light on role drug discovery development. By offering comprehensive overview recent advancements both synthesis this will serve as valuable resource for researchers practitioners navigating evolving landscape medicinal chemistry.

Язык: Английский

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Synthesis of new fluorinated sulfonates and their Schiff bases as anti-Alzheimer drug candidates: An in vitro-in silico study

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141474 - 141474

Опубликована: Янв. 1, 2025

Язык: Английский

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BACE-1 Inhibitors Targeting Alzheimer's Disease

Current Alzheimer Research, Год журнала: 2023, Номер 20(3), С. 131 - 148

Опубликована: Март 1, 2023

The accumulation of amyloid-β (Aβ) is the main event related to Alzheimer's disease (AD) progression. Over years, several disease-modulating approaches have been reported, but without clinical success. amyloid cascade hypothesis evolved and proposed essential targets such as tau protein aggregation modulation β-secretase (β-site precursor cleaving enzyme 1 - BACE-1) γ-secretase proteases. BACE-1 cuts (APP) release C99 fragment, giving rise Aβ peptide species during subsequent cleavage. In this way, has emerged a clinically validated attractive target in medicinal chemistry, it plays crucial role rate generation. review, we report results candidates trials E2609, MK8931, AZD-3293, addition highlighting pharmacokinetic pharmacodynamic-related effects inhibitors already reported. current status developing new peptidomimetic, non-peptidomimetic, naturally occurring, other class are demonstrated, considering their limitations lessons learned. goal provide broad complete approach subject, exploring chemical classes perspectives.

Язык: Английский

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Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: Current and future perspective

RSC Medicinal Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Дек. 6, 2024

This review collates the recent information related to proposed hypotheses for AD etiology and advances in various therapeutic options, with a particular emphasis on clinical candidates.

Язык: Английский

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[3+2] Cycloaddition Synthesis of New Piperazine‐Linked Bis(chromene) Hybrids Possessing Pyrazole Units as Potential Acetylcholinesterase Inhibitors

Chemistry & Biodiversity, Год журнала: 2023, Номер 20(4)

Опубликована: Март 29, 2023

Two series of piperazine-linked bis(chromene) hybrids that are attached to pyrazole units were synthesized in the current study. Both an acyl unit at pyrazole-C3, with one acetyl and other ethoxycarbonyl unit. A [3+2] cycloaddition protocol was conducted produce target good yields by reacting appropriate hydrazonoyl chlorides chromene-based bis(enaminone) dioxane containing triethylamine reflux for 4 h. New tested acetylcholinesterase inhibitory activity concentrations 15 25 μM, as well their ability quench 2,2-diphenylpicrylhydrazyl (DPPH) free radicals a concentration μg/mL. In general, is related electronic properties para-substituent arene pyrazole-N1. Furthermore, pyrazole-C3 has significant effect on new hybrids' activity. At previous concentrations, (3-acetylpyrazole)-linked hybrid p-NO2 demonstrated best activity, inhibition percentages 79.7 90.2. most effective DPPH percentage 87.5.

Язык: Английский

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The literature of heterocyclic chemistry, part XXII, 2022

Advances in heterocyclic chemistry, Год журнала: 2025, Номер unknown

Опубликована: Янв. 1, 2025

Язык: Английский

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