Microwave-Assisted Semisynthesis and Leishmanicidal Activity of Some Phenolic Constituents from Lichens
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Archivos
Fecha
2023-10
Profesor/a Guía
Facultad/escuela
Idioma
en
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Título del volumen
Editor
Multidisciplinary Digital Publishing Institute (MDPI)
Nombre de Curso
Licencia CC
CC BY 4.0 DEED
Attribution 4.0 International
Licencia CC
https://creativecommons.org/licenses/by/4.0/
Resumen
Leishmaniasis is considered one of the most untreated tropical diseases in the world. In this study, we investigated the in vitro leishmanicidal activity and cytotoxicity of various isolated lichen substances, including atranorin (1), usnic acid (2), gyrophoric acid (3), salazinic acid (4), galbinic acid (5), and parietin (6), and some semi-synthetic imine derivatives of usnic acid (7, 8, 9) and atranorin (10, 11, 12, 13). Imine condensation reactions with hydrazine and several amines were assisted by microwave heating, an efficient and eco-friendly energy source. The most interesting result was obtained for compound 2, which has high leishmanicidal activity but also high cytotoxicity. This cytotoxicity was mitigated in its derivative, 9, with better selectivity and high antileishmanic activity. This result may indicate that the usnic acid derivative (9) obtained using condensation with two cyclohexylamine groups is a promising lead compound for the discovery of new semisynthetic antiparasitic drugs. © 2023 by the authors.
Notas
INDEXACIÓN: SCOPUS.
Palabras clave
atranorin derivatives, cytotoxicity, green chemistry, imine, leishmania, pyrazoline, usnic acid derivatives
Citación
Separations, Volume 10, Issue 10, October 2023, Article number 524
DOI
10.3390/separations10100524