SYNTHESIS OF NEW N-ALKYL-2-BENZYLTHIOPYRIMIDINE DERIVATIVES AND CONCENTRATIONS INFLUENCE ON MULTIRESISTANT BACTERIA GROWTH

2021 
Synthesis and study of new N-alkyl-2-benzylsulfanyl-pyrimidines concentration influences on multidrug resistant bacteria growth are presented in this article. This novel series are compounds 3a-k derived from 1-ethyl or 1-benzyl-2- benzylsulfanyl -6-methyl-4-phenyl-1,4- dihydropyrimidine-5-carboxylates. They were obtained by condensation reaction between 2- benzylsulfanyl-pyrimidines (1) and benzyl chloride or ethyl bromide (2) in the presence of potassium carbonate (K2CO3). The compounds synthesized were characterized by 1H, 13C Nuclear Magnetic Resonance (NMR) spectra and High-Resolution Mass Spectrometry (HRMS). Among these compounds, ten were evaluated for their potential antibacterial activity on multidrug-resistant strains of Escherichia coli and Staphylococcus aureus. The results showed a negative influence against the tested bacteria growth. Compounds 3b, 3d, 3f, 3h, 3e and 3k were more potent on S. aureus with IC50 ranging from 6.04 to 28.59 µg / mL The compounds 3b, 3c, 3f, 3g, 3h and 3j were more active on E. coli with IC50 between 7.21 and 26.59 µg / mL.
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