Malaria continues to pose a significant global health and socio-economic burden on those regions where it is endemic. Despite substantial investment in the delivery of artemisinin-based combination therapies, causing a fall in malaria mortality, recent data suggest that this parasitic disease still imposes a significant impact. A major problem is the narrow drug discovery pipeline, made worse by reports of artemisinin resistance. In recent years, high-throughput screening of natural products derived from plants and marine organisms has led to the discovery of potent anti-malarial indole alkaloids (such as dihydrousambarensine), many of which contain an indoloisoquinoline core. Building on previously discovered methodology in our group, we have developed a series of novel, enantiomerically pure, synthetic indoloisoquinoline and their potential as anti-malarial leads was assessed. The structure-activity relationship of these compounds was investigated in several areas and a lead compound was generated with an activity close to that of a known anti-malarial natural product dihydrousambarensine.
| Identifer | oai:union.ndltd.org:bl.uk/oai:ethos.bl.uk:638507 |
| Date | January 2013 |
| Creators | Fallon, Samantha Kate |
| Publisher | Keele University |
| Source Sets | Ethos UK |
| Detected Language | English |
| Type | Electronic Thesis or Dissertation |
| Source | http://eprints.keele.ac.uk/196/ |
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