Pharmaceutical Chemistry Journal, Год журнала: 2024, Номер 58(7), С. 1069 - 1083
Опубликована: Окт. 1, 2024
Язык: Английский
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
Процитировано
3
Talanta, Год журнала: 2025, Номер 287, С. 127574 - 127574
Опубликована: Янв. 11, 2025
Язык: Английский
Процитировано
2
European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 273, С. 116523 - 116523
Опубликована: Май 21, 2024
Язык: Английский
Процитировано
12
Ageing Research Reviews, Год журнала: 2024, Номер 97, С. 102298 - 102298
Опубликована: Апрель 10, 2024
Язык: Английский
Процитировано
9
Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141474 - 141474
Опубликована: Янв. 1, 2025
Язык: Английский
Процитировано
1
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
Процитировано
7
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
Процитировано
13
Advances in heterocyclic chemistry, Год журнала: 2025, Номер unknown
Опубликована: Янв. 1, 2025
Язык: Английский
Процитировано
0
ACS Chemical Neuroscience, Год журнала: 2025, Номер unknown
Опубликована: Март 19, 2025
The cholinergic deficits and deposition of β-amyloid (Aβ) species are regarded as the key events contributing to progression Alzheimer's disease (AD). Herein, a series novel donor-acceptor architecture-type potential theranostic agents were designed, synthesized, evaluated for their against cholinesterase (ChE) enzymes detection Aβ species, which primary targets in development therapeutics AD. optimal compound/probe 18 containing benzothiazolium fluorophore with bifunctional electron-donating N-aryl piperazine scaffold exhibited potent inhibitory activities acetylcholinesterase (AChE; IC50 = 0.172 ± 0.011 μM) butyrylcholinesterase (BuChE; 1.376 0.141 μM). Measurement fluorescence properties showed that probe emission maxima (λem) >610 nm dimethyl sulfoxide (DMSO) >590 PBS, suitable imaging. In vitro studies demonstrated change characteristics high binding affinities (18; Kd 0.731 upon aggregates. affinity toward aggregates was further observed elavGAL4 > UAS Aβ, Drosophila larval brain sections, using imaging technique. vivo acute oral toxicity evaluation indicated safety profile lead 18. Moreover, behavioral including Y-maze object recognition tests signified administration compound improved cognitive spatial memory impairment at dose 10 20 mg/kg scopolamine-induced deficit model.
Язык: Английский
Процитировано
0
Medicinal Chemistry Research, Год журнала: 2025, Номер unknown
Опубликована: Апрель 18, 2025
Язык: Английский
Процитировано
0