Abstract
Thiourea derivatives (1–38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02–91.50 ± 0.08 μM, most of which are superior to the standard thiourea (IC50 = 21.00 ± 0.11 μM). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 μM.
[Display omitted] Compounds 1–38 showed a varying degree or urease inhibitory activities with IC50 values in the range of 5.53 ± 0.02–91.50 ± 0.08 μM, most of which are superior compared to the standard.
•Synthesis of N,N'-disubstituted thiourea derivatives.•In vitro urease inhibitory activity.•Thirteen compounds found to be the most active.•Structure–activity relationship has been established.