Antimalarials based on the arylpiperazine privileged substructure

Based on a previous study, arylpiperazines (2-chlorophenylpiperazine, 2-ethoxyphenylpiperazine and phenylpiperazine) were found to be significantly more potent against the chloroquine-resistant (K1) strain than against the chloroquine-sensitive(DIO) strain. In other studies, 8-hydroxy-2-(di-n-propylamino)tetralin (8-0H-DPAT) has been identified as a potential antimalarial agent for the inhibition of the 5-hydroxytryptamine type 1A receptor in Plasmodium falciparum. A number of arylpiperazines are also known to target this receptor in other systems. Coupled with the potential role of arylpiperazines as replacements for the antimalarial 8-OH-OPA T, these results prompted a further investigation into the antiplasmodial properties of a broader range of simple un substituted and substituted arylpiperazines against a broader range of chloroquine-sensitive and chloroquine-resistant strains of PlasmodiumJalciparum.

Grantor dc:publisher.institution

Department of Chemistry

Year dc:date.issued

2005

Author dc:creator

• Molyneaux, Carrie-Anne

Advisor dc:contributor.advisor

• Chibale, Kelly

Language dc:language.iso

eng

Handle dc:identifier.uri

http://hdl.handle.net/11427/6342

OAI identifier oai:identifier

oai:open.uct.ac.za:11427/6342