10.4067/S0717-97072012000200014
The study explores a convenient method for synthesizing substituted benzimidazoles using Trimethylsilyl Chloride (TMSCl) as a catalyst in a microwave-induced two-phase system. The chemicals involved include o-phenylenediamine and various carboxylic acids as starting materials, TMSCl as the catalyst, and solvents such as DMF and water. The TMSCl catalyzes the cyclization of o-phenylenediamine with carboxylic acids to form benzimidazoles. The microwave conditions significantly reduce reaction time and enhance yield compared to conventional heating methods. The synthesized compounds were evaluated for their in vitro antibacterial and antifungal activities against several pathogenic strains, revealing that certain compounds, such as 3e, 3f, 3g, 3k, 3m, 3n, and 3o, demonstrated antimicrobial activity comparable to standard drugs like ampicillin and itraconazole, with the most effective compounds showing activity at a MIC of 6.25 μg/mL. The study concludes that the presence of a substituted phenyl ring at position 2 of the benzimidazole structure might be responsible for the enhanced antimicrobial activity.
