Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline

Eur J Med Chem. 2008 Oct;43(10):2045-55. doi: 10.1016/j.ejmech.2007.11.003.

Sandrine Delarue-Cochin ¹, Philippe Grellier, Louis Maes, Elisabeth Mouray, Christian Sergheraert, Patricia Melnyk

Affiliations

Affiliation

1 UMR CNRS 8525, Université de Lille II, Institut Pasteur de Lille, 1 rue du Professeur Calmette, B.P. 447, 59021 Lille cedex, France.

PMID: 18226428 DOI: 10.1016/j.ejmech.2007.11.003

Abstract

A series of 4-anilinoquinolines bearing an amino side chain linked to the aromatic ring with a carbamate or an amide bond were synthesized and evaluated for their antimalarial activity and their cytotoxicity upon MRC-5 cells. Among the 17 compounds, a majority was found to be active in the low nanomolar range against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro with relative low cytotoxicity. Two compounds were then tested on mice infected by Plasmodium berghei and were found to exhibit reasonable in vivo activity.

Name
Email *

	Sorry, but the email address you supplied was invalid.