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Future Med Chem ; 11(24): 3109-3124, 2019 12.
Artículo en Inglés | MEDLINE | ID: mdl-31838897

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.


Asunto(s)
Abietanos/síntesis química , Antibacterianos/síntesis química , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Abietanos/química , Abietanos/farmacología , Abietanos/toxicidad , Antibacterianos/química , Antibacterianos/farmacología , Antibacterianos/toxicidad , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Aberraciones Cromosómicas/inducido químicamente , Eritrocitos/efectos de los fármacos , Hemólisis/efectos de los fármacos , Humanos , Leucocitos Mononucleares/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Cebollas/efectos de los fármacos , Cebollas/genética , Relación Estructura-Actividad
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