Synthesis and structure–activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus

CHABÁN, MACARENA FUNES; I ANTONIOU, ANTONIA; KARAGIANNI, CATHERINE; TOUMPA, DIMITRA; JORAY, MARIANA BELÉN; BOCCO, JOSÉ LUIS; SOLA, CLAUDIA; M ATHANASSOPOULOS, CONSTANTINOS; CARPINELLA, MARÍA CECILIA

Future Medicinal Chemistry

Future Science and Newlands Press

Lugar: London; Año: 2019 vol. 11 p. 3109 - 3109

1756-8919

im: 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.