Back to Search
Start Over
Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2021 Nov 23; Vol. 26 (23). Date of Electronic Publication: 2021 Nov 23. - Publication Year :
- 2021
-
Abstract
- 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.
- Subjects :
- Acetophenones chemical synthesis
Biological Products chemical synthesis
Cell Survival drug effects
Chagas Disease parasitology
Chalcones chemical synthesis
Chromones chemical synthesis
Flavones chemical synthesis
Humans
Trypanocidal Agents chemical synthesis
U937 Cells
Acetophenones pharmacology
Biological Products pharmacology
Chagas Disease metabolism
Chalcones pharmacology
Chromones pharmacology
Drug Discovery methods
Flavones pharmacology
Trypanocidal Agents pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 26
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 34885649
- Full Text :
- https://doi.org/10.3390/molecules26237067