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Synthesis, antiprotozoal and antibacterial activity of nitro- and halogeno-substituted benzimidazole derivatives.

Acta biochimica Polonica (2002-07-26)
Zygmunt Kazimierczuk, Jacqueline A Upcroft, Peter Upcroft, Agata Górska, Bohdan Starościak, Agnieszka Laudy
RÉSUMÉ

Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia, and an activity comparable to that of metronidazole against gram-positive and gram-negative bacteria. Of the tested compounds, 5,6-dichloro-2-(4-nitrobenzylthio)-benzimidazole showed the most distinct antiprotozoal activity.

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Sigma-Aldrich
2-Chloro-N,N-diethylethylamine hydrochloride, 99%
Sigma-Aldrich
3,4-Dichlorobenzyl chloride, 97%