TITLE:
New Sulfonamides Derived from Carvacrol: Compounds with High Antibacterial Activity against Resistant Staphylococcus aureus Strains
AUTHORS:
Aldo Sena de Oliveira, Luana Canzian Llanes, Inês Maria Costa Brighente, Ricardo José Nunes, Rosendo Augusto Yunes, Nilton Máximo Junior, Ana Milda Karsten Baumgart, Anays Noumeh Aust, Alexandre Bella Cruz
KEYWORDS:
Sulfonamides, Carvacrol, Antibacterial, Staphylococcus aureus, Synergism
JOURNAL NAME:
Journal of Biosciences and Medicines,
Vol.4 No.7,
July
20,
2016
ABSTRACT: Nine new sulfonamides
derived from carvacrol were prepared through a reaction between 4-hydroxy-2-isopropyl-5-methyl benzene sulfonyl
chloride with various amines in excellent yields (76% - 92%). The sulfonamides
were characterized using spectrometric and spectroscopic methods. Among these
compounds, three derivatives showed excellent results in antibacterial activity
against resistant S. aureus strains, with MIC values ranging from 3.9 to
62.50 ppm. The sulfonamide derivative of 4-methylaniline (SULF-1) had the best
performance for all tested strains of bacteria (MIC = 3.9 to 15.62 ppm).
Furthermore, the sulfonamide derivative of 4-fluoro aniline (SULF-3), which
also presented promising results, was found to have a synergistic effect when
combined with tetracycline and partial synergistic effect when combined with
ampicillin, exhibiting an FIC index between 0.50 and 0.75. The sulfonamide
derivative of 4-methylaniline had a synergistic effect in combination with
erythromycin exhibiting an FIC index of 0.37. Carvacrol in association with the
antibiotics tested did not have a synergistic effect.