Abstract
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).Graphical
Highlights
Microorganisms play a key role in the functioning of the environment but they are a real threat to human life and health
The unequivocal reports regarding the scale of pathogenic microbial resistance to commonly used drugs have forced the search for new antimicrobial agents (Coates et al 2002; Spellberg et al 2008; Llor and Bjerrum 2014)
In our current research we focused our attention on both Mannich bases and pipemidic acid
Summary
Microorganisms play a key role in the functioning of the environment but they are a real threat to human life and health. The unequivocal reports regarding the scale of pathogenic microbial resistance to commonly used drugs have forced the search for new antimicrobial agents (Coates et al 2002; Spellberg et al 2008; Llor and Bjerrum 2014)
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