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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.
- 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.
- Subjects :
- Animals
Antimalarials chemistry
Antimalarials pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Chloroquine pharmacology
Drug Resistance
Female
Humans
Malaria drug therapy
Mice
Piperazines chemistry
Piperazines pharmacology
Plasmodium berghei
Plasmodium falciparum drug effects
Quinolines chemistry
Quinolines pharmacology
Structure-Activity Relationship
Tumor Cells, Cultured
Antimalarials chemical synthesis
Piperazines chemical synthesis
Quinolines chemical synthesis
Subjects
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