Design and synthesis of novel synthetic and natural product inspired trypanosomatid inhibitors

  • Rodrigo Pierre Freire De Araujo Gouy

Student thesis: Doctoral Thesis (PhD)


Chapter 1 – Introduction of neglected tropical diseases, their impact in our society, treatments,
and current challenges. We further explore how a limited understanding of these diseases
impedes their treatments. Identification of novel compounds and targets as well as
repurposing of previously developed promising drug candidates, may lead to improvement of
current treatments methods.

Chapter 2 – Nitro heteroaromatic compounds have demonstrated their potential through their
recurrent use as antiparasitic treatments. The novel series of nitro containing heteroaromatics
moieties presented in this work were designed to further explore their antiparasitic potential
and improve the series for the use in target identification studies.

Chapter 3 – Fumagillin, a natural product isolated from Aspergillus fumigatus, has recently
been found to be a promising antiparasitic drug candidate. Its target in mammalian cell lines
has been found to be the enzyme MetAP2, however its target in trypanosomatids parasite is
yet to be confirmed. In this chapter, we discuss the development of a new series of fumagillin
analogues with increased antiparasitic potential. The determined SAR is further applied in the
synthesis of probes for imaging and photo-affinity labelling suitable for target identification.

Chapter 4 – Summary of the synthesised compounds for both series and biological data
obtained throughout this work, and discussion of further work on both series towards novel
analogues with antiparasitic potential.
Date of Award30 Jun 2021
Original languageEnglish
Awarding Institution
  • University of St Andrews
SupervisorGordon John Florence (Supervisor)


  • Neglected tropical diseases
  • Trypanosomiasis
  • Natural products
  • Fumagillin
  • Nitro heteroaromatic
  • Target identification

Access Status

  • Full text embargoed until
  • 9th April 2024

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