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Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

Authors :
Ryckebusch A
Deprez-Poulain R
Maes L
Debreu-Fontaine MA
Mouray E
Grellier P
Sergheraert C
Source :
Journal of medicinal chemistry [J Med Chem] 2003 Feb 13; Vol. 46 (4), pp. 542-57.
Publication Year :
2003

Abstract

Three series of monoquinolines consisting of a 1,4-bis(3-aminopropyl)piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and one of them cured mice infected by Plasmodium berghei.

Details

Language :
English
ISSN :
0022-2623
Volume :
46
Issue :
4
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
12570376
Full Text :
https://doi.org/10.1021/jm020960r