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Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype
The blood stage of the malarial parasite life-cycle is a vital stage that is believed to be a target for most antimalarial drugs. It is in this stage that host haemoglobin is degraded to provide nutrients for the survival of the parasite. However, a pathway (known as the haem detoxification pathway)...
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| Format: | Thesis |
| Language: | English |
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Department of Chemistry
2015
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| _version_ | 1867613188705484800 |
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| access_status_str | Open Access |
| author | Mvumvu, Nomakhwezi |
| author2 | Egan, Timothy J |
| author_browse | Egan, Timothy J Mvumvu, Nomakhwezi |
| author_facet | Egan, Timothy J Mvumvu, Nomakhwezi |
| author_sort | Mvumvu, Nomakhwezi |
| collection | Thesis |
| description | The blood stage of the malarial parasite life-cycle is a vital stage that is believed to be a target for most antimalarial drugs. It is in this stage that host haemoglobin is degraded to provide nutrients for the survival of the parasite. However, a pathway (known as the haem detoxification pathway) that gives rise to the unique, microcrystalline ferriprotoporphryin IX [Fe(III)PPIX] dimer called haemozoin as an end-product, also arises as a result of the degradation. This haem detoxification pathway is a principal target for some of these antimalarials, especially those that contain the quinoline scaffold (e.g chloroquine), and has yielded outstanding results for the antimalarial drug discovery and development world. Even so, the spread of parasite resistance among these drugs has rendered most ineffective, resulting in a need for new scaffolds to target the pathway. However, the mode of action of chloroquine on haem may still be used as a model for identification of hits from these new scaffolds. |
| format | Thesis |
| id | oai:open.uct.ac.za:11427/15743 |
| institution | University of Cape Town (South Africa) |
| language | eng |
| last_indexed | 2026-06-10T12:32:11.035Z |
| license_str | Not specified — see source repository |
| provenance_str_mv | Harvested via OAI-PMH from UCTD — University of Cape Town Open Access Repository |
| publishDate | 2015 |
| publishDateRange | 2015 |
| publishDateSort | 2015 |
| publisher | Department of Chemistry |
| publisherStr | Department of Chemistry |
| record_format | dspace |
| source_str | UCTD — University of Cape Town Open Access Repository |
| spelling | oai:open.uct.ac.za:11427/15743 Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype Mvumvu, Nomakhwezi Egan, Timothy J Hunter, Roger Chemistry The blood stage of the malarial parasite life-cycle is a vital stage that is believed to be a target for most antimalarial drugs. It is in this stage that host haemoglobin is degraded to provide nutrients for the survival of the parasite. However, a pathway (known as the haem detoxification pathway) that gives rise to the unique, microcrystalline ferriprotoporphryin IX [Fe(III)PPIX] dimer called haemozoin as an end-product, also arises as a result of the degradation. This haem detoxification pathway is a principal target for some of these antimalarials, especially those that contain the quinoline scaffold (e.g chloroquine), and has yielded outstanding results for the antimalarial drug discovery and development world. Even so, the spread of parasite resistance among these drugs has rendered most ineffective, resulting in a need for new scaffolds to target the pathway. However, the mode of action of chloroquine on haem may still be used as a model for identification of hits from these new scaffolds. 2015-12-09T14:47:09Z 2015-12-09T14:47:09Z 2015 Master Thesis Masters MSc http://hdl.handle.net/11427/15743 eng application/pdf Department of Chemistry Faculty of Science University of Cape Town |
| spellingShingle | Chemistry Mvumvu, Nomakhwezi Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| thesis_degree_str | Master's |
| title | Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| title_full | Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| title_fullStr | Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| title_full_unstemmed | Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| title_short | Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype |
| title_sort | synthesis of 1 4 dihydropyridines as potential antimalarial chemotype |
| topic | Chemistry |
| url | http://hdl.handle.net/11427/15743 |
| work_keys_str_mv | AT mvumvunomakhwezi synthesisof14dihydropyridinesaspotentialantimalarialchemotype |