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

Autor: Luis A. González, Sara Robledo, Yulieth Upegui, Gustavo Escobar, Wiston Quiñones
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Molecules, Vol 26, Iss 23, p 7067 (2021)
Druh dokumentu: article
ISSN: 26237067
1420-3049
DOI: 10.3390/molecules26237067
Popis: 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.
Databáze: Directory of Open Access Journals
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