Chiba, Diego Eidy; dos Santos Fernandes, Guilherme Felipe; dos Santos, Jean Leandro; Scarim, Cauê Benito; (2024) Exploring the latest breakthroughs in rhodesain inhibitors for African trypanosomiasis. Medicinal Chemistry Research 10.1007/s00044-024-03189-0. (In press).

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Abstract

Human African Trypanosomiasis is a serious public health concern, and new chemical therapeutic agents need to be developed to combat this disease. Rhodesain (RhD) inhibitors have shown promising results in medicinal chemistry, specifically against Trypanosoma brucei. These inhibitors target the cysteine protease RhD, which is essential for the survival of T. brucei. However, as the pharmaceutical industry lacks interest in these inhibitors, the development of drugs based on them is challenging. In this review, we showed the impact of RhD inhibitors on medicinal chemistry in the past 10 years (2013–2022), particularly against T. brucei, showing interesting RhD-based inhibitors, including peptidomimetic inhibitors such as Michael acceptors, cyanide groups, 3-bromoisoxazole, benzodiazepine, among others, as well as non-peptidyl inhibitors. Peptidomimetic inhibitors (5–7, 9–15, and 17) exhibited the highest potency with respect to dissociation constant (Ki) values for rhodesain, demonstrating promising activity against T. brucei targeting rhodesain. Thus, we explored recent advancements and perspectives in the context of RhD for potential treatments in sleeping sickness, highlighting its relevance in drug discovery applications.

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