- Title
- Synthesis, characterization and in vitro antiplasmodial evaluation of 4-& 8-aminoquinoline based-hybrid compounds
- Creator
- Nqoro, Xhamla
- Subject
- Plasmodium falciparum
- Date Issued
- 2018
- Date
- 2018
- Type
- Thesis
- Type
- Masters
- Type
- MSc
- Identifier
- http://hdl.handle.net/10353/14649
- Identifier
- vital:40026
- Description
- Malaria is a deadly disease and its drug resistance has been reported to be a challenge globally. The death toll caused by malaria has increased rapidly in different regions of the world. Quinoline scaffold molecules are combined with other classes of antimalarials to tackle drug resistance. The combination of quinoline scaffolds with other antimalarial compounds and metals-based drugs have been reported to be a potential approach to overcome drug resistance common in the currently used antimalarials. 4-Aminoquinoline was hybridized with selected organic molecules and metal-based compounds to form a class of hybrid compounds containing either an amide bond or ester bond as a linker between the parent molecules. 4-Aminoquinoline derivatives are known compounds and they were prepared via known synthetic routes and characterized. The hybrid compounds were characterized and the FTIR results confirmed the successful linkage of 4-aminoquinoline derivatives to selected organic scaffolds to form hybrid compounds. NMR results confirmed the successful formation of hybrid compounds. MS showed signals of the hybrid molecules confirming the successful isolation of the hybrid compounds. In vitro antiplasmodial assay was performed against asexual parasite and chloroquine was used as a reference drug. The percentage inhibition effects of the hybrid compounds were in a range of 96-102% at 5 µM and 36-96% at 1 µM suggesting that the percentage inhibition effect of the hybrid compounds was influenced by the drug concentration. Hybridization of either 4-aminosalicylic scaffold or ferrocene butanoic acid with 4- aminoquinoline derivatives is a potential synthetic route that can result in potent antimalarials. However, more research is needed to fully understand the structure-activity relationship of these hybrid compounds.
- Format
- 125 leaves
- Format
- Publisher
- University of Fort Hare
- Publisher
- Faculty of Science and Agriculture
- Language
- English
- Rights
- University of Fort Hare
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UFH Department of Chemistry
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Nqoro_201300305_dissertation new.pdf | 3 MB | Adobe Acrobat PDF | View Details Download |