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Synthesis and in vitro antimicrobial activity screening of new pipemidic acid derivatives
Łukasz Popiołek,Anna Biernasiuk,Kinga Paruch,Anna Malm,Monika Wujec 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.6
This article describes the synthesis and antimicrobialactivity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis ofMannich reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with pipemidic acid. Antimicrobial tests revealedhigh antibacterial activity of obtained derivatives. Gramnegativerods belonging to Enterobacteriaceae family wereparticularly most sensitive to new pipemidic acid derivatives. Synthesized compounds exhibited very strongactivity towards Proteus mirabilis ATCC 12453,Salmonella typhimurium ATCC 14028 and Escherichia coliATCC 25922. The minimum inhibitory concentrations ofnew pipemidic acid derivatives which inhibited the growthof these bacteria were 0.98–7.81 μg/ml, 0.98–7.81 μg/mland 0.98–3.91 μg/ml, respectively. The antibacterialactivity of newly synthesized pipemidic acid derivatives inmany cases was far better than the activity of substancesused as positive controls (nitrofurantoin, cefuroxime,ampicillin and pipemidic acid).