Prodrugs of antiparasitic redox-active compounds

For many years, redox-active compounds have been considered unspecific and dangerous although they have a tremendous potential as drugs as exemplified with old drugs in the past. The ambition of our 4-year project entitled FeROS, is to break through dogmatic and conceptual barriers by designing novel efficient and safe boron-based prodrugs of redox medicines with innovative modes of action. As a proof of concept, we aim to deliver preclinical leads in the family of para-naphthol-derived benzoxaboroles and boronic acids, with highly specific antiparasitic activities against parasites causing malaria (MAL), Chagas disease (CD), leishmaniasis (LSH) and schistosomiasis (SCH).

FeROS is a project aiming to achieve validation and demonstration of effective and specific drugs against multiple protozoan and metazoan parasites, ready to deliver for pre-clinical studies for the treatment of these diseases. A new class of antiparasitic drugs would not only improve the health of millions of people, but also impact the economy of endemic low- and middle-income countries, where these diseases result in considerable morbidity and mortality among vulnerable populations, and limit the (re)emergence of these diseases in Europe due to population movements (war, climate, economy exiles) and climatic changes.

FeROS will also provide an understanding of the molecular mechanism underlying prodrug activation and redox-active drug killing mechanisms. By designing boron-based prodrugs of redox compounds as potent and specific medicines against infectious diseases, FeROS will offer a technological breakthrough in medicinal chemistry and pharmaceutical industry.