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Eur J Med Chem ; 95: 473-82, 2015 May 05.
Artigo em Inglês | MEDLINE | ID: mdl-25847765

RESUMO

A series of phenylpropanoid derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the synthesized derivatives showed effective anti-HBV activity. Of these compounds, compound 4c-1 showed the most potent anti-HBV activity, demonstrating potent inhibitory effect not only on the secretion of HBsAg (IC50 = 14.18 µM, SI = 17.85) and HBeAg (IC50 = 6.20 µM, SI = 40.82) secretion but also HBV DNA replication (IC50 = 23.43 µM, SI = 10.80). The structure-activity relationships (SARs) of phenylpropanoid derivatives had been discussed, which were useful for phenylpropanoid derivatives to be explored and developed as novel anti-HBV agents. Moreover, the docking study of all synthesized compounds inside the HLA-A protein (PDB ID: 3OX8) active site were carried out to explore the molecular interactions and a molecular target for activity of phenylpropanoid derivatives with the protein using a moe-docking technique. This study identified a new class of potent anti-HBV agents.


Assuntos
Antivirais/síntese química , Antivirais/farmacologia , Desenho de Fármacos , Vírus da Hepatite B/efeitos dos fármacos , Fenóis/síntese química , Fenóis/farmacologia , Antivirais/química , Antivirais/metabolismo , Domínio Catalítico , Técnicas de Química Sintética , Replicação do DNA/efeitos dos fármacos , Antígenos HLA-A/química , Antígenos HLA-A/metabolismo , Células Hep G2 , Antígenos de Superfície da Hepatite B/metabolismo , Antígenos E da Hepatite B/metabolismo , Vírus da Hepatite B/metabolismo , Vírus da Hepatite B/fisiologia , Humanos , Simulação de Acoplamento Molecular , Fenóis/química , Fenóis/metabolismo , Relação Quantitativa Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
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