Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides
Braz. J. Pharm. Sci. (Online)
;
53(1): e16067, 2017. tab, graf
Artículo
en Inglés
| 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:
Disponible
Índice:
LILACS (Américas)
Asunto principal:
Leishmaniasis
/
Relación Estructura-Actividad Cuantitativa
Tipo de estudio:
Estudio pronóstico
Límite:
Animales
Idioma:
Inglés
Revista:
Braz. J. Pharm. Sci. (Online)
Asunto de la revista:
Farmacologia
/
Teraputica
/
Toxicologia
Año:
2017
Tipo del documento:
Artículo
País de afiliación:
Brasil
Institución/País de afiliación:
Universidade Federal de Minas Gerais/BR
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