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.
Langmuir ; 33(39): 10351-10365, 2017 10 03.
Artigo em Inglês | MEDLINE | ID: mdl-28895402

RESUMO

It has been long known that the physical encapsulation of oleic acid-capped iron oxide nanoparticles (OA-IONPs) with the cetyltrimethylammonium (CTA+) surfactant induces the formation of spherical iron oxide nanoparticle clusters (IONPCs). However, the behavior and functional properties of IONPCs in chemical reactions have been largely neglected and are still not well-understood. Herein, we report an unconventional ligand-exchange function of IONPCs activated when dispersed in an ethyl acetate/acetate buffer system. The ligand exchange can successfully transform hydrophobic OA-IONP building blocks of IONPCs into highly hydrophilic, acetate-capped iron oxide nanoparticles (Ac-IONPs). More importantly, we demonstrate that the addition of silica precursors (tetraethyl orthosilicate and 3-aminopropyltriethoxysilane) to the acetate/oleate ligand-exchange reaction of the IONPs induces the disassembly of the IONPCs into monodispersed iron oxide-acetate-silica core-shell-shell (IONPs@acetate@SiO2) nanoparticles. Our observations evidence that the formation of IONPs@acetate@SiO2 nanoparticles is initiated by a unique micellar fusion mechanism between the Pickering-type emulsions of IONPCs and nanoemulsions of silica precursors formed under ethyl acetate buffered conditions. A dynamic rearrangement of the CTA+-oleate bilayer on the IONPC surfaces is proposed to be responsible for the templating process of the silica shells around the individual IONPs. In comparison to previously reported methods in the literature, our work provides a much more detailed experimental evidence of the silica-coating mechanism in a nanoemulsion system. Overall, ethyl acetate is proven to be a very efficient agent for an effortless preparation of monodispersed IONPs@acetate@SiO2 and hydrophilic Ac-IONPs from IONPCs.

2.
Bioorg Med Chem Lett ; 19(3): 1009-11, 2009 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-19101144

RESUMO

Compilation of agmatine structure and imidazoline ring leads to a new family of imidazoline/alpha(2)-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. Constraining of the guanidine moiety into heterocyclic ring improved the affinities of the resultant fusion compounds in comparison to agmatine itself. In this work, the synthetic approach and results for I(1), I(2), and alpha(2)-adrenoceptors affinities are reported.


Assuntos
Agmatina/análogos & derivados , Química Farmacêutica/métodos , Receptores de Imidazolinas/química , Agmatina/farmacologia , Clonidina/farmacologia , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Guanidina/química , Humanos , Imidazóis , Receptores de Imidazolinas/metabolismo , Concentração Inibidora 50 , Cinética , Modelos Químicos , Ligação Proteica , Receptores Adrenérgicos alfa 2/metabolismo , Proteínas Recombinantes de Fusão/química
3.
J Enzyme Inhib Med Chem ; 20(2): 115-21, 2005 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15968815

RESUMO

A series of N-acyl peptides 1-9, containing an inhibitor of glucosamine-6-phosphate synthase have been synthesised and tested against Candida strains. N-Acylated peptides inhibit glucosamine-6-phosphate synthase in cell free extracts from Candida albicans. Antifungal activities of the tested compounds correlated with their lipophilic properties. Peptides acylated with decanoic acid were found to be the most potent in the series. N-decanoylpeptides also showed activity against Candida albicans Gu5 resistant mutant with Cdr1 and Cdr2 drug extrusion proteins that causes MDR by an active efflux mechanism.


Assuntos
Antifúngicos/farmacologia , Candida albicans/metabolismo , Candidíase/tratamento farmacológico , Farmacorresistência Fúngica , Inibidores Enzimáticos/farmacologia , Glutamina-Frutose-6-Fosfato Transaminase (Isomerizante)/antagonistas & inibidores , Peptídeos/farmacologia , Sistema Livre de Células , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/síntese química , Células HL-60 , Humanos , Técnicas In Vitro , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Modelos Químicos , Mutação , Peptídeos/síntese química , Peptídeos/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA