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Indian Journal of Chemistry -Section B (IJC-B) >
IJC-B Vol.50B [2011] >
IJC-B Vol.50B(02) [February 2011] >
| 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 |
| CC License: |  CC Attribution-Noncommercial-No Derivative Works 2.5 India |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Source: | IJC-B Vol.50B(02) [February 2011]
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