Thiazolidinones and related analogues as efficient antitrypanosomal agents

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F25%3A73632451" target="_blank" >RIV/61989592:15310/25:73632451 - isvavai.cz</a>
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0968089625003049" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0968089625003049</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2025.118363" target="_blank" >10.1016/j.bmc.2025.118363</a>

Result language
angličtina
Original language name
Thiazolidinones and related analogues as efficient antitrypanosomal agents
Original language description
We designed and synthesised a series of thiazolidinediones and related analogues and evaluated their antiparasitic activity. A structure-activity relationship (SAR) study focused on modifications of specific parts of the molecule revealed derivatives that displayed significant activity against Trypanosoma brucei species. Notably, the analogue 6i exhibited exceptional activity, with an EC50 value of 30 nM and a selectivity index of >2000, against the protozoan Trypanosoma brucei rhodesiense, which causes human African trypanosomiasis. Additionally, compounds 6a, 6k, 7e, and 16 demonstrated antitrypanosomal activities in the less than 5 μM range. Our most active analogue 6i represents a promising candidate for further preclinical development.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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