Fallon, Samantha Kate (2013) Development of new heterocyclic leads against malaria. Doctoral thesis, Keele University.
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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.
|Item Type:||Thesis (Doctoral)|
|Uncontrolled Keywords:||anti-malarial drugs, disease,|
|Subjects:||R Medicine > RS Pharmacy and materia medica|
|Divisions:||Faculty of Medicine and Health Sciences > Institute for Science and Technology in Medicine|
|Depositing User:||Michael Debenham|
|Date Deposited:||09 Dec 2014 14:13|
|Last Modified:||09 Dec 2014 14:13|
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