No abstract

A series of 7-piperazinylquinolones containing a (benzo[d]imidazol-2-yl)methyl moiety were designed and synthesized as new antibacterial agents. The antibacterial activity of title compounds was evaluated against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia) microorganisms. Among the tested compounds, the N1-cyclopropyl derivative 4a showed the highest activity against S. aureus, S. epidermidis, B. subtilis and E. coli ([Formula: see text] [Formula: see text]g/mL), being 2-4 times more potent than reference drug norfloxacin. A structure-activity relationship study demonstrated that the effect of the nitro group on the benzimidazole ring depends on the pattern of substitutions on the piperazinylquinolone.

Background: Trichomonas vaginalis infectious disease is an important worldwide health problem. Although, several drugs especially metronidazole and tinidazole have been used in the treatment, their-resistant strains have been developed and unpleasant adverse effects exist. Garlic and other Allium species are old medicinal plants, which were used for infectious diseases, cardiovascular disorders and hair and skin cosmetic diseases. Objectives: We aimed to compare the anti-trichomoniasis activities of three species of Allium. Methods: The Trichomonas vaginalis strain was isolated from vaginal discharge of women with vaginitis symptoms and cultured in a modified TYM medium. After confirmation of herbarium of the plants, their extracts were prepared. For testing, 24 sterile plates were used. In all 24 homes, 200 µL of TYM were poured out. The tube containing the parasite, counting the number of angels with the aid of Neubauer slide and set to 500,000 per mL, was added to the amount of 100 µL to all wells. In order to investigate the antitrichomoniasis of the plant, concentrations of 37.5, 75, 150, 300, 600, 1200 and 2400 µg/mL of extract have been tested. For positive control, 50 mL of metronidazole, 50 µg/mL, was added to culture medium. In addition to, no herbal extract and metronidazole was added to the well of negative control. Results: The leaf extract of bell circus with a concentration of 2000 µg/mL after 48 hours and boiled cabbage bulb onion at a concentration of 24 µg/mL and leaf extract of turmericum at a concentration of 1500 µg/mL in 48 hours and boiled horseradish onions at 48 µg/mL concentration in 24 hours could achieve 100% GI and significantly inhibit parasite growth. Leaf extract, boiled onions and essential oils inhibited the growth of Trichomonas parasites, were not as high as 100%. Conclusions: According to the results obtained in our study, these Allium plants have inhibitory activity on growth of Trichomonas vaginalis parasite.