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Oxazolopyridines towards the treatment of Human African sleeping sickness


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Almohaywi, B 2014 , 'Oxazolopyridines towards the treatment of Human African sleeping sickness', Research Master thesis, University of Tasmania.

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This thesis describes the synthesis and structure activity relationship (SAR) of
oxazolopyridine and related analogues against Trypanosoma brucei, the causative agent of
Human African Trypanosomiasis, a neglected, fatal parasitic disease that is a major cause of
death and disability affecting many sub-Saharan African countries.
Collaborators at Monash Institute of Pharmaceutical Science (MIPs), and ESKITIS institute
found eight compounds as potential candidates via high throughput screening (HTS) of a
large library of compounds against the disease. Amongst the compounds screened, an
oxazolo[4,5-b]pyridine compound was of particular interest. In collaboration with MIPS, this
work aimed to modify certain regions of the lead compounds and to develop a SAR against T.
brucei, aiming for the synthesis of better analogues of the lead compound, as discussed in
Chapter 2 and Chapter 3. A number of compounds have been made through modification
around the central phenyl ring and the heterocyclic oxazolopyridine core. Modification at the
central phenyl ring revealed the intolerance of that position for substitution, while the best
compounds remained either the lead compound itself or its analogues, with the chlorine being
replaced by either a hydrogen or substituting the 2-furyl amide for its 3-furyl counterpart.
Modification of the heterocyclic core has resulted in a number of active compounds. We
suggested that the modification and substitutions on oxazolopyridine core is more favourable
for better activity. In addition to the anti-trypanosomal activities, these compounds are similar to heterocyclic
amine derivatives found in cooked meat and fish, which has the potential to cause cancer.
This has prompted us to investigate the potential for DNA damage activity of these
compounds and the amine precursors, as discussed in Chapter 4.

Item Type: Thesis - Research Master
Authors/Creators:Almohaywi, B
Keywords: oxazolopyridine, Trypanosoma brucei, Human African Trypanosomiasis, Monash Institute of Pharmaceutical Science (MIPs),
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