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Hazelton, J.C., Iddon, B., Suschitzky, H. and Woolley, L.H. (1995) 2H-Benzimidazoles (Isobenzimidazoles). Part 10. Synthesis of Polysubstituted O-Phenylenediamines and Their Conversion into Heterocycles, Particularly 2-Substituted Benzimidazoles with Known or Potential Anthelminthic Activity. Tetrahedron, 51, 10771-10794.
https://doi.org/10.1016/0040-4020(95)00642-L

has been cited by the following article:

• TITLE: Design, Synthesis and in Vitro Antibacterial Activity of 2-thiomethyl-benzimidazole Derivatives

  AUTHORS: Ablo Evrard, Coulibali Siomenan, Camara Tchambaga Etienne, Toure Daouda, Coulibaly Souleymane, Sissouma Drissa, Adjou Ané

  KEYWORDS: Antibacterial Activity, Benzimidazole, 2-Methylbenzimidazole Thiouronium, Halide

  JOURNAL NAME: Advances in Biological Chemistry, Vol.11 No.4, August 27, 2021

  ABSTRACT: 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).