Artículo
Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus
Funes Chabán, Macarena
; Antoniou, Antonia I.; Karagianni, Catherine; Toumpa, Dimitra; Joray, Mariana Belén
; Bocco, Jose Luis
; Sola, Claudia del Valle
; Athanassopoulos, Constantinos; Carpinella, Maria Cecilia
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Fecha de publicación:
12/2019
Editorial:
Future Medicine Ltd.
Revista:
Future Medicinal Chemistry
ISSN:
1756-8919
e-ISSN:
1756-8927
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
To find alternative compounds against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA), novel derivatives from dehydroabietic acid were synthesized. Methods & results: Compound 12 was the most effective against 15 MRSA and 11 MSSA with minimum inhibitory concentration values ranging from 3.9 to 15.6 μg/ml. Although less active than 12, compound 11, followed by 25 and 13, also exhibited anti-staphylococcal activity. Additional studies showed that compound 12 is devoid of toxic effect on non-target cells. A structure-activity relationship study revealed that an oxime at C-13 together with a hydroxyl at C-12 could play a key role in the activity. Conclusion: These structures, in particular compound 12, could arise as templates for the development of agents against MRSA and MSSA.
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Articulos(IRNASUS)
Articulos de INSTITUTO DE INVESTIGACIONES EN RECURSOS NATURALES Y SUSTENTABILIDAD JOSE SANCHEZ LABRADOR S.J.
Articulos de INSTITUTO DE INVESTIGACIONES EN RECURSOS NATURALES Y SUSTENTABILIDAD JOSE SANCHEZ LABRADOR S.J.
Citación
Funes Chabán, Macarena; Antoniou, Antonia I.; Karagianni, Catherine; Toumpa, Dimitra; Joray, Mariana Belén; et al.; Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus; Future Medicine Ltd.; Future Medicinal Chemistry; 11; 24; 12-2019; 3109-3124
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