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Title: Synthesis and antimalarial activity of novel N-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-7-chloroquinolin-4-amine and its derivatives
Authors: Tanwar, Pooja
Yadav, Gyan Chand
Jaitley, U K
Kaushik, Naveen
Sahal, Dinkar
Keywords: Antimalarial;4-aminoquinoline;Heteroalkane¬amine-quinolines;Alkyl ether substituted quinolines
Issue Date: Feb-2011
Publisher: NISCAIR-CSIR, India
Abstract: A number of N-{2-[2-(2-aminoethoxy)ethoxy]ethyl}-7-chloroquinolin-4-amine derivatives have been prepared by condensation of N-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-7-chloroquinolin-4-amine with substituted aldehyde. The newly synthesized compounds have been characterized by IR, ¹H and ¹³C NMR, and mass spectral data. These compounds have been screened for in vitro antimalarial activity using the Sybr Green assay of P. falciparum in culture and the heme detoxification based Heme-HRP assay. Among these, compounds 7-chloro-N-[2-(2-{2-[(2, 4-difluorobenzyl) amino] ethoxy} ethoxy) ethyl] quinolin-4-amine is found to be the most effective with IC50 value 60 M (in Heme-HRP assay) and 48 nM (in P. falciparum culture assay). These values compare well with the potency of chloroquine in the respective assays.
Page(s): 233-241
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.50B(02) [February 2011]

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