info:eu-repo/semantics/article
Efficient multicomponent synthesis of diverse antibacterial embelin-privileged structure conjugates
Fecha
2020-07Registro en:
Martín Acosta, Pedro; Peña, Rosalyn; Feresin, Gabriela Egly; Tapia, Alejandro; Lorenzo Castrillejo, Isabel; et al.; Efficient multicomponent synthesis of diverse antibacterial embelin-privileged structure conjugates; Molecular Diversity Preservation International; Molecules; 25; 14; 7-2020; 1-22
1420-3049
CONICET Digital
CONICET
Autor
Martín Acosta, Pedro
Peña, Rosalyn
Feresin, Gabriela Egly
Tapia, Alejandro
Lorenzo Castrillejo, Isabel
Machín, Félix
Amesty, Ángel
Estévez Braun, Ana
Resumen
A library of embelin derivatives has been synthesized through a multicomponent reaction from embelin (1), aldehydes and privileged structures such as 4-hydroxycoumarin, 4-hydroxy-2H-pyran-2-one and 2-naphthol, in the presence of InCl3 as catalyst. This multicomponent reaction implies Knoevenagel condensation, Michael addition, intramolecular cyclization and dehydration. Many of the synthesized compounds were active and selective against Gram-positive bacteria, including one important multiresistant Staphylococcus aureus clinical isolate. It was found how the conjugation of diverse privileged substructure with embelin led to adducts having enhanced antibacterial activities.