Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones.

Luis A González, Sara Robledo, Yulieth Upegui, Gustavo Escobar, Wiston Quiñones

Molecules (Basel, Switzerland) 2021 Nov 23

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American trypanosomiasis (Chagas disease) caused by the Trypanosoma cruzi parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process. Some acetophenones and chalcones, as well as chromane-type substances, such as chromones and flavones, are natural products that have been studied as trypanocides, but the relationships between structure and activity are not yet fully understood. In this work, 26 compounds were synthesized to determine the effect of hydroxyl and isoprenyl substituents on trypanocide activity. One of the compounds showed interesting activity against a resistant strain of T. cruzi, with a half effective concentration of 18.3 µM ± 1.1 and an index of selectivity > 10.9.

Citation

Luis A González, Sara Robledo, Yulieth Upegui, Gustavo Escobar, Wiston Quiñones. Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones. Molecules (Basel, Switzerland). 2021 Nov 23;26(23)