Parasitic infections caused by protozoa remain one of the main contributors to fatalities in developing countries, but also contribute to the disease burden in emerging countries. Certain Trypanosomatida are human pathogens that cause a variety of vector-borne parasitic diseases, such as Chagas disease, leishmaniasis, and sleeping sickness. While no vaccines are available to date, the current treatment options are limited and suffer from severe adverse effects and growing resistance. The paullones, a family of protein kinase inhibitors, have been shown to exhibit antitrypanosomal activity by inhibiting TryS (trypanothione synthetase), a unique and essential ATP-dependent enzyme of the thiol-redox metabolism of Trypanosomatida. Our project focuses on identifying secondary targets of this compound class and to study the role and fate of these inhibitors inside the parasite cell. To that end, we report our progress synthesizing and characterizing rationally designed fluorescent conjugates of paullones using organic fluorophores. These labelled compounds will be evaluated as chemical probes in in vitro and in cellulo studies using fluorescence-based techniques.

Design, synthesis and evaluation of fluorescent derivatives of antitrypanosomal paullones

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ACS Fall 2022

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