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Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-sub- stituted 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.
The objective of the present study that has been carried out in the Institute of Chemistry, Warsaw University of Life Sciences, was to investigate antimicrobial activity of a number of sweet marjoram extracts. Raw (fresh or dried) plant material from culinary or medicinal herbs may contain varying amounts of bacteria or protozoa, including some known human pathogens. The isolates, which are prepared by procedures involving the use of elevated temperature and/or organic solvents or other chemicals are expected to have considerably less or no such potentially harmful burden. Four sweet marjoram (Origanum majorana L.) fractions obtained by steam distillation, Soxhlet n-hexane extraction, extraction with aqueous ethanol, and with ethanolic ammonia solution were evaluated in vitro for activity against twenty Gram-positive or Gram-negative bacterial strains, six Candida sp. yeast strains and a single protozoan species Pentatrichomonas hominis. The n-hexane extract showed the highest antibacterial activity and inhibited growth of eight out of nine Staphylococcus aureus strains used. The other bacteria showed no substantial susceptibility to the extracts, except that Acinetobacter baumannii showed some inhibition by the aqueous ethanol extract. The isolates were also active against three out of six Candida sp. strains used, and the ethanolic ammonia extract reduced the number of viable P. hominis trophozoites by 50% at 160 µg·ml-1 concentration in 24 h cultures; the remaining extracts were considerably less or but marginally effective. These data warrant further study on identifying the components of the extracts with the highest activities.
Benzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position 5-, namely 5-chloro-4-(1H-benzimidazole-2-yl)phenol (Cpd I), 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) and 4-(1H-benzimidazole-2-yl)phenol (Cpd III), were synthesized and evaluated for their effects on mammalian type I DNA topoisomerase activity using quantitative in vitro plasmid supercoil relaxation assays. For the structure elucidation of the compounds, melting points, UV, IR, 1H NMR, 13C NMR, mass spectral data and elemental analyses were interpreted. Among the compounds, 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) manifested relatively potent topoisomerase I inhibition.
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