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Synthesis and in vitro antimicrobial activity screening of new pipemidic acid derivatives

Popiołek, Łukasz, Biernasiuk, Anna, Paruch, Kinga, Malm, Anna, Wujec, Monika
Archives of pharmacal research 2018 v.41 no.6 pp. 633-645
Escherichia coli, Gram-negative bacteria, Proteus mirabilis, Salmonella Typhimurium, ampicillin, antibacterial properties, cefuroxime, minimum inhibitory concentration, nitrofurantoin, screening
This article describes the synthesis and antimicrobial activity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis of Mannich reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with pipemidic acid. Antimicrobial tests revealed high antibacterial activity of obtained derivatives. Gram-negative rods belonging to Enterobacteriaceae family were particularly most sensitive to new pipemidic acid derivatives. Synthesized compounds exhibited very strong activity towards Proteus mirabilis ATCC 12453, Salmonella typhimurium ATCC 14028 and Escherichia coli ATCC 25922. The minimum inhibitory concentrations of new pipemidic acid derivatives which inhibited the growth of these bacteria were 0.98–7.81 µg/ml, 0.98–7.81 µg/ml and 0.98–3.91 µg/ml, respectively. The antibacterial activity of newly synthesized pipemidic acid derivatives in many cases was far better than the activity of substances used as positive controls (nitrofurantoin, cefuroxime, ampicillin and pipemidic acid).