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

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.

Bibliographic Details

Main Authors:	Lavorato,Stefânia Neiva, Duarte,Mariana Costa, Andrade,Pedro Henrique Rocha De, Coelho,Eduardo Antonio Ferraz, Alves,Ricardo José
Format:	Digital revista
Language:	English
Published:	Universidade de São Paulo, Faculdade de Ciências Farmacêuticas 2017
Online Access:	http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100620
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