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Title: Development of new heterocyclic leads against malaria
Author: Fallon, Samantha Kate
Awarding Body: Keele University
Current Institution: Keele University
Date of Award: 2013
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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.
Supervisor: Not available Sponsor: Not available
Qualification Name: Thesis (Ph.D.) Qualification Level: Doctoral
EThOS ID:  DOI: Not available
Keywords: RS Pharmacy and materia medica