Author(s)

Ablo Evrard¹, Coulibali Siomenan^1*, Camara Tchambaga Etienne¹, Toure Daouda², Coulibaly Souleymane¹, Sissouma Drissa¹, Adjou Ané¹

¹Laboratoire de Constitution et Réaction de la Matière, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphouët Boigny de Cocody, Abidjan, Côte d’Ivoire.
²Département de Biologie, UFR des Sciences Biologiques, Université Peleforo Gon Coulibaly, Korhogo, Côte d’Ivoire.

A series of novel substituted benzimidazole (7a - n) derivatives were synthesized and characterized by ¹H, ¹³C Nuclear Magnetic Resonance (NMR) spectra and High Resolution Mass Spectrometry (HRMS). The substitution was done in position -1 and -2 by appropriate groups. These compounds are obtained by N-alkylation reaction with thiomethyl-1H-benzimidazole intermediates (5a - g). Design of intermediates (5a - g) was made by condensation reaction between 2-methylbenzimidazole thiourunium salt (3) and functionalized halides (4) in the presence of sodium hydroxide (NaOH). Among the twenty-one compounds synthesized, ten were evaluated for their antimicrobial activity on three bacterial strains namely: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853. Only E. coli ATTC 25922 was susceptible to the synthesized derivatives 5g, 7f and 7h with a significant antibacterial activity (CMI is between 250 and 500 μg/mL).

Antibacterial Activity, Benzimidazole, 2-Methylbenzimidazole Thiouronium, Halide

Evrard, A. , Siomenan, C. , Etienne, C. , Daouda, T. , Souleymane, C. , Drissa, S. and Ané, A. (2021) Design, Synthesis and in Vitro Antibacterial Activity of 2-thiomethyl-benzimidazole Derivatives. Advances in Biological Chemistry, 11, 165-177. doi: 10.4236/abc.2021.114012.