N -monosubstituted thiosemicarbazide as novel Ure inhibitors: synthesis, biological evaluation and molecular docking.
In: Future medicinal chemistry, Jg. 12 (2020-09-01), Heft 18, S. 1633-1645
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Zugriff:
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.
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N -monosubstituted thiosemicarbazide as novel Ure inhibitors: synthesis, biological evaluation and molecular docking.
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Autor/in / Beteiligte Person: | Ni, WW ; Fang, HL ; Ye, YX ; Li, WY ; Yuan, CP ; Li, DD ; Mao, SJ ; Li, SE ; Zhu, QH ; Ouyang, H ; Xiao, ZP ; Zhu, HL |
Zeitschrift: | Future medicinal chemistry, Jg. 12 (2020-09-01), Heft 18, S. 1633-1645 |
Veröffentlichung: | London : Future Science, 2009-, 2020 |
Medientyp: | academicJournal |
ISSN: | 1756-8927 (electronic) |
DOI: | 10.4155/fmc-2020-0048 |
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