info:eu-repo/semantics/article
Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus
Fecha
2019-12Registro en:
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
1756-8919
1756-8927
CONICET Digital
CONICET
Autor
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
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.