Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 3 de 3
Filtrar
Mais filtros

Base de dados
Tipo de documento
País de afiliação
Intervalo de ano de publicação
1.
J Org Chem ; 87(2): 1325-1334, 2022 01 21.
Artigo em Inglês | MEDLINE | ID: mdl-35007075

RESUMO

An asymmetric synthetic route to (-)-galanthamine (1), a pharmacologically active Amaryllidaceae alkaloid used for the symptomatic treatment of early onset Alzheimer's disease, was successfully established with very high levels of stereocontrol. The key to achieving high chemo- and stereo-selectivity in this approach was the use of transition-metal-mediated reactions, namely, enyne ring-closing metathesis, Heck coupling, and titanium-based asymmetric allylation.


Assuntos
Alcaloides , Doença de Alzheimer , Galantamina , Humanos
2.
Spectrochim Acta A Mol Biomol Spectrosc ; 308: 123783, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38134654

RESUMO

In this study, two fluorescent sensing probes, dihydropyridine (DHP) derivatives (DHP-CT1 and DHP-CT2) bearing phenoxy thiocarbonyl group, have been developed for Hg2+ detection. The tandem trimerization-cyclization of methylpropiolate with ammonium acetate gave 1.4-DHP and 1,2-DHP derivatives, which were reacted with O-phenylcarbonochloridothioate to produce DHP-CT1 and DHP-CT2, respectively. DHP-CT1 exhibits superior sensitivity and selectivity of fluorescence enhancement towards Hg2+ in aqueous media. The fluorescence intensity shows a good linear relationship with the concentration of Hg2+ in the range of 0-10 µM providing the extremely low LOD of 346 nM (69.4 ppb). The fluorescence enhancement is caused by the Hg2+ promoted hydrolysis of the thioamide bond releasing the fluorescent 1,4-DHP that was confirmed by NMR and HRMS. The quantitative analysis of Hg2+ in water samples using DHP-CT1 probe was demonstrated in aqueous solution and paper-based sensing strips. Furthermore, DHP-CT1 was also applied for monitoring intracellular Hg2+ in living RAW264.7 macrophages through fluorescence cell imaging.


Assuntos
Corantes Fluorescentes , Mercúrio , Corantes Fluorescentes/química , Água , Espectrometria de Fluorescência/métodos , Espectroscopia de Ressonância Magnética , Mercúrio/análise
3.
Bioorg Med Chem Lett ; 23(10): 2880-2, 2013 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-23583510

RESUMO

The synthesis of racemic tetrahydrocurcumin- (THC-), tetrahydrodemethoxycurcumin- (THDC-) and tetrahydrobisdemethoxycurcumin- (THBDC-) dihydropyrimidinone (DHPM) analogues was achieved by utilizing the multi-component Biginelli reaction in the presence of copper sulphate as a catalyst. The evaluation of acetylcholinesterase inhibitors for Alzheimer's disease of these compounds showed that they exhibited higher inhibitory activity than their parent analogues. THBDC-DHPM demonstrated the most potent inhibitory activity with an IC50 value of 1.34±0.03µM which was more active than the approved drug galanthamine (IC50=1.45±0.04µM).


Assuntos
Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Curcumina/análogos & derivados , Curcumina/farmacologia , Pirimidinas/farmacologia , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Curcumina/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Pirimidinas/química , Estereoisomerismo , Relação Estrutura-Atividade
SELEÇÃO DE REFERÊNCIAS
Detalhe da pesquisa