Pyrazole and its derivatives are becoming increasingly prevalent in medicine due to their proven antimicrobial activity. The development of new derivatives increases the likelihood of discovering new effective antibiotics. The pyrazole derivative, 4-(2-aminoethyl)-1-(pyridine-2-yl)-1H-pyrazole-5-ol (I1), inhibits the growth of Escherichia coli and L-threonine dehydrogenase (TDH) activity. The enzyme is a key component in amino acid metabolism and biofilm formation. TDH is not present in humans nor does it have a homologous protein in humans, hence I1 could be a potential base for new drug development. The aim of the research project was to examine the different types of pyrazole derivatives and their effects on TDH activity and whether they affect the formation of biofilms. For the enzyme to work, the cofactor NAD+ is required, where upon the reaction is converted into NADH, which then makes it possible for fluorometric detection of activity. Among the tested derivatives, I1 was the most promising and potent. Derivative I2 also had similar inhibitory activity. However, due to its poor solubility, it proved impossible to test at higher concentrations. Tests were also conducted to see the impact derivatives have on biofilm formation, and the results showed that all derivatives inhibit biofilm formation. However, only I1 and I2 directly affect TDH activity. Based on these findings, further research is required to establish with certainty to prove the correlation between TDH inhibition and biofilm formation suppression.
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