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Future Med Chem ; 13(12): 1025-1039, 2021 06.
Artículo en Inglés | MEDLINE | ID: mdl-33928790

RESUMEN

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36-39 exhibited potent antibacterial activity against HA-MRSA, with MIC = 8-64 µg/ml. Additionally, a combination of compound 37 and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Conclusion: Compound 37 has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.


Asunto(s)
Antibacterianos/farmacología , Diseño de Fármacos , Ginsenósidos/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Compuestos de Nitrógeno/farmacología , Compuestos Policíclicos/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Ginsenósidos/síntesis química , Ginsenósidos/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Compuestos de Nitrógeno/química , Compuestos Policíclicos/química
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