Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 33, Issue 3, Pages 247-263Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2023.2193328
Keywords
Trypanosoma brucei; cysteine protease; inhibitors; dihydrofolate reductase; pterine reductase 1; oxaborole analogues; fusaricidin A; human African trypanosomiasis
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This review provides an overview of the recent advances in the discovery of new inhibitors and biological targets for the treatment of Human African Trypanosomiasis. It also discusses the development of new vaccines and formulations. The findings of this study are valuable for the search of new therapeutic options for this neglected disease.
IntroductionHuman African Trypanosomiasis is a neglected disease caused by infection from parasites belonging to the Trypanosoma brucei species. Only six drugs are currently available and employed depending on the stage of the infection: pentamidine, suramin, melarsoprol, eflornithine, nifurtimox, and fexinidazole. Joint research projects were launched in an attempt to find new therapeutic options for this severe and often lethal disease.Areas coveredAfter a brief description of the recent literature on the parasite and the disease, we searched for patents dealing with the proposal of new antitrypanosomiasis agents and, following the PRISMA guidelines, we filtered the results to those published from 2018 onwards returning suitable entries, which represent the contemporary landscape of compounds/strategies against Trypanosoma brucei. In addition, some relevant publications from the overall scientific literature were also discussed.Expert opinionThis review comprehensively covers and analyzes the most recent advances not only in the discovery of new inhibitors and their structure-activity relationships but also in the assessment of innovative biological targets opening new scenarios in the MedChem field. Finally, also new vaccines and formulations recently patented were described. However, natural and synthetic compounds were analyzed in terms of inhibitory activity and selective toxicity against human cells.
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