Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas

Eur J Med Chem. 2014 Mar 3:74:314-23. doi: 10.1016/j.ejmech.2014.01.001. Epub 2014 Jan 14.

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.

Keywords: In vitro urease inhibition activity; Kinetic study; Synthesis; Thiourea derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Thiourea / pharmacokinetics
  • Thiourea / pharmacology*
  • Urease / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Urease
  • Thiourea