Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides
Braz. J. Pharm. Sci. (Online)
;
53(1): e16067, 2017. tab, graf
Artigo
em Inglês
| LILACS
| ID: biblio-839450
ABSTRACT
ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity.
Texto completo:
DisponíveL
Índice:
LILACS (Américas)
Assunto principal:
Leishmaniose
/
Relação Quantitativa Estrutura-Atividade
Tipo de estudo:
Estudo prognóstico
Limite:
Animais
Idioma:
Inglês
Revista:
Braz. J. Pharm. Sci. (Online)
Assunto da revista:
Farmacologia
/
Teraputica
/
Toxicologia
Ano de publicação:
2017
Tipo de documento:
Artigo
País de afiliação:
Brasil
Instituição/País de afiliação:
Universidade Federal de Minas Gerais/BR
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