Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

AUTOR(ES)

Lavorato, Stefânia Neiva, Duarte, Mariana Costa, Andrade, Pedro Henrique Rocha De, Coelho, Eduardo Antonio Ferraz, Alves, Ricardo José

FONTE

Braz. J. Pharm. Sci.

DATA DE PUBLICAÇÃO

20/04/2017

RESUMO

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.

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