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- W3083531389 abstract "Background: Identification of novel Ure inhibitors with high potency has received considerable attention. Methodology & results: Ure inhibition was determined using the indophenol method, the affinities to Ure were estimated via surface plasmon resonance. Seventeen new plus ten known N-monosubstituted thiosemicarbazides were synthesized and identified as novel Ure inhibitors. Out of these compounds, compound b5 shows excellent activity against both crude Ure from Helicobacter pylori (IC 50 = 0.04 μM) and Ure in living cell (IC 50 = 0.27 μM), with the potency being over 600-fold higher than clinical used drug acetohyroxamic acid, respectively. Surface plasmon resonance demonstrated the high affinity ( K d .#x00A0;= 6.32 nM) of b5 to Ure. Conclusion: This work provides a class of novel and promising Ure inhibitors." @default.
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- W3083531389 date "2020-09-01" @default.
- W3083531389 modified "2023-10-13" @default.
- W3083531389 title "<i>N</i>-monosubstituted thiosemicarbazide as novel Ure inhibitors: synthesis, biological evaluation and molecular docking" @default.
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- W3083531389 doi "https://doi.org/10.4155/fmc-2020-0048" @default.
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