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Design, synthesis and biological evaluation of novel α-aminoamide derivatives / 国际药学研究杂志
Journal of International Pharmaceutical Research ; (6): 560-565, 2020.
Artigo em Chinês | WPRIM | ID: wpr-845161
ABSTRACT

Objective:

To design and synthesize novel α-aminoamide derivatives for the treatment of neuropathic pain.

Methods:

Ralfinamide was used as a lead compound, and it's ring A was replaced by a benzoheterocyclic moiety(2, 3-dihydrobenzofuran or 2, 3-dihydrobenzo[b][1, 4]dioxin)to obtain the new compounds 5a-5f. The in vivo and in vitro analgesic activities of the new compounds were evaluated by the formalin test and the whole-cell patch clamp assay, respectively.

Results:

In the formalin test in vivo, compound 5e exhibited higher analgesic activities(60% higher)than ralfinamide(P<0.05). The whole-cell patch clamp assay showed that the inhibitory effect of all tested compounds, except for 5d, on sodium channel Nav1.7 was much weaker than ralfinamide (P<0.05 or P<0.01).

Conclusion:

A set of new compounds with better analgesic activities than ralfinamide were obtained via optimizing the structure of ring A of ralfinamide. The reults of this study can provide useful references for relative research.

Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Idioma: Chinês Revista: Journal of International Pharmaceutical Research Ano de publicação: 2020 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Idioma: Chinês Revista: Journal of International Pharmaceutical Research Ano de publicação: 2020 Tipo de documento: Artigo