Fallon, Samantha Kate (2013) Development of new heterocyclic leads against malaria. Doctoral thesis, Keele University.

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Abstract

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
URI: http://eprints.keele.ac.uk/id/eprint/196

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