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Wang, Y., Inguaggiato, G., Jasamai, M., Shah, M., Hughes, D., Slater, M. and Simons, C. (1999) Synthesis and Biological Evaluation of Novel 2’-deoxy-4’-thio-imidazole Nucleosides. Bioorganic & Medicinal Chemistry, 7, 481-487.
https://doi.org/10.1016/S0968-0896(98)00255-7

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).