నైరూప్య

Influence of N-methyl piperidine on Antibacterial Activity of 2-(thioalkyl)-1Hmethylbenzimidazole Derivatives

Coulibaly Souleymane, Coulibali Siomenan, Ablo Evrard, Coulibaly Bakary, Camara Tchambaga Etienne and Adjou Ane

Antibiotic resistance becomes a public health issue nowadays. The overcoming and settlement of this ongoing crisis could be to find novel, potent, and selective antimicrobial agents. For that we synthesized 2-(thioalkyl)-1H-methylbenzimidazole derivatives (3a-g) by S-alkylation, and added piperidine via Mannich reaction to yield 2-(thioalkyl)-methyl-1-(piperidin-1-ylmethyl) benzimidazole derivatives (4a-g). The antimicrobial profiles of both derivatives were first estimated by their inhibition diameters and determined with Minimal Inhibitory Concentrations (MICs) against a small set of bacteria clinical strains of Escherichia coli, Klebsiella pneumoniae (Gram-negative bacteria), Staphylococcus aureus and Pseudomonas aeruginosa (Gram-positive bacteria). The panel of synthesized compounds (3a-g) and (4a-g) were characterized by NMR 1H, 13C spectroscopy, and high-resolution mass spectrometry (HRMS). The results revealed that compounds 3a and 3b, were both bactericidal on P. aeruginosa and E. coli with a great MIC value of 1µg/mL. Then the addition of piperidine show promising inhibition diameter but did not implement the bactericidal activity in terms of MIC on P. aeruginosa.