Alkylation of 2-aminobenzimidazole by methyliodide and benzyl- or 2-aryloxyethylbromides produced 1-substituted 2-aminobenzimidazoles that were quaternized by chloroacetamide to previously undescribed 3-aryloxyethyl(benzyl)-1-carbamoylmethyl-2-iminobenzimidazoline hydrochlorides. These compounds were shown to possess antibacterial activity against several pathogenic Gram-positive and Gram-negative microbes (Staphylococcus aureus, Escherichia coli) combined with pronounced protistocidal activity against the protozoa Colpoda steinii that was on the level of the clinical reference drugs.
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The work used equipment at the CCU “Molecular spectroscopy” of the IPOC, SFU, and was performed in part under the auspices of State Task, Project No. 4.196.2014/K.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 48, No. 10, pp. 29 – 32, October, 2014.
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Divaeva, L.N., Morkovnik, A.S., Zubenko, A.A. et al. Synthesis, Antimicrobial, and Protisticidal Activity of 3-Aryloxyethyl(Benzyl)-1-Carbamoylmethyl-2-Iminobenzimidazoline Hydrochlorides. Pharm Chem J 48, 661–664 (2015). https://doi.org/10.1007/s11094-015-1165-4
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DOI: https://doi.org/10.1007/s11094-015-1165-4