首页|4-Aminoquinoline-ferrocene Hybrids as Potential Antimalarials

4-Aminoquinoline-ferrocene Hybrids as Potential Antimalarials

扫码查看
Background: Malaria is a deadly disease. It is mostly treated using 4-aminoquinoline derivatives such as chloroquine etc. because it is well-tolerated, displays low toxicity, and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for the treatment of malaria. Furthermore, some patents reported hybrids 4-aminoquinolines containing ferrocene moiety with potent antimalarial activity. Objective: The objective of the current study is to prepare 4-aminoquinoline-ferrocene hybrids via esterification and amidation reactions. The compounds were characterized via FTIR, LC-MS and NMR spectroscopy. In vitro screening against chloroquine-sensitive P. falciparum parasite (NF54) at concentrations (1 muM and 5 muM) and an inhibitory concentration (full dose-response) was studied. Methods: The compounds were prepared via known reactions and monitored by Thin Layer Chromatography. The compounds were purified by column chromatography and characterized using FTIR, NMR and MS. In vitro antiplasmodial evaluation was performed against asexual parasite and chloroquine was used as a reference drug.

FerrocenePlasmodium falciparum4-aminoquinolineesterification reactionhybrid compoundmalaria.

Xhamla Nqoro Blessing A. Aderibigbe

展开 >

Department of Chemistry, University of Fort Hare, Alice Campus, Alice, South Africa

2020

Recent patents on anti-infective drug discovery.

Recent patents on anti-infective drug discovery.

ISSN:1574-891X
年,卷(期):2020.15(2)
  • 2