-monosubstituted thiosemicarbazide as novel Ure inhibitors: synthesis, biological evaluation and molecular docking.

Identification of novel Ure inhibitors with high potency has received considerable attention. Ure inhibition was determined using the indophenol method, the affinities to Ure were estimated via surface plasmon resonance. Seventeen new plus ten known -monosubstituted thiosemicarbazides were synthesized and identified as novel Ure inhibitors. Out of these compounds, compound shows excellent activity against both crude Ure from (IC = 0.04 μM) and Ure in living cell (IC = 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 (.#x00A0;= 6.32 nM) of to Ure. This work provides a class of novel and promising Ure inhibitors.