Synthesis and effect of N-alkylation on antibacterial activity of 2-(Benzylthio) methyl-1H-benzimidazole derivatives

In pursuit the development of novel potent and selective antibacterial agents, we synthesized twelve (12) N-alkyl 2-benzylthiomethyl-1H-benzimidazole derivatives evaluated their activities. Their profile was determined with minimal inhibitory concentrations (MICs) minimum bactericidal (MBCs) against a small set two (2) strains Escherichia coli (Gram negative) Staphylococcus aureus positive). These compounds are produced by condensation reaction (5) benzyl chloride or bromide (6) in presence potassium carbonate (K2CO3). The panel synthetized (7a-l) were characterized NMR 1H, 13C spectroscopy, high-resolution mass spectrometry (HRMS). results showed that 7a, 7b, 7c, 7d, 7e, 7f, 7h, 7k, 7l aureus, significant MICs values from 140 to 290 µg/mL. On E. coli, five 7i, 7k effects within common an N-alkylation R3= phenyl, methyl, CH2OH on benzimidazole scaffold benzylthiol substituted R2= Cl CF3. This is evidence probe these chemical groups implementing activity.