Envíe este artículo por correo electrónico Heterochalconas de pirazina “sobre-agua”: enfoque bioisostérico y su actividad antimicrobiana in vitro
Resumen
Se sintetizaron cinco heterochalconas (PI-1 a PI-5) mediante reacción de Claisen-Schmidt “sobre-agua”, un sistema heterogéneo con sustratos insolubles y base miscible, alcanzando rendimientos de 67 a 79%. La elucidación estructural se realizó por RMN 1H y 13C. La actividad antimicrobiana se evaluó frente a Staphylococcus aureus, Candida albicans y Escherichia coli, observán-dose inhibición solo en las dos primeras. Los halos de inhibición fueron mayores en C. albicans (12,2 ± 0,3 a 23,4 ± 0,6 mm) que en S. aureus (10,2 ± 0,6 a 16,7 ± 0,9 mm). Los bioisósteros clásicos (sustitución de hidrogeno por flúor) aumentaron la eficiencia farmacológica, mientras que los no clásicos (fenil por pirrol) la redujeron.
Recibido: 29/08/2025
Aceptado: 19/11/2025
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