Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides
Braz. J. Pharm. Sci. (Online)
; 53(1): e16067, 2017. tab, graf
Article
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| LILACS
| ID: biblio-839450
Biblioteca responsable:
BR1.1
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.
Palabras clave
Texto completo:
1
Bases de datos:
LILACS
Asunto principal:
Leishmaniasis
/
Relación Estructura-Actividad Cuantitativa
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
Braz. J. Pharm. Sci. (Online)
Asunto de la revista:
Farmacologia
/
Teraputica
/
Toxicologia
Año:
2017
Tipo del documento:
Article
País de afiliación:
Brasil