INVESTIGADORES
CARPINELLA Maria Cecilia
artículos
Título:
Synthesis and structure-activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus
Autor/es:
FUNES CHABÁN M.; ANTONIOU A.I.; KARAGIANNI C.A.; TOUMPA D.; JORAY M.B.; BOCCO J.L.; SOLA C.; ATHANASSOPOULOS C.M.; CARPINELLA M. C.
Revista:
Future Medicinal Chemistry
Editorial:
Future Science
Referencias:
Año: 2019 vol. 11 p. 3109 - 3124
ISSN:
1756-8919
Resumen:
Aim: 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.
