Synthesis and in vitro urease inhibitory activity of N,N′-disubstituted thioureas
2014; Elsevier BV; Volume: 74; Linguagem: Inglês
10.1016/j.ejmech.2014.01.001
ISSN1768-3254
AutoresKhalid Mohammed Khan, Farzana Naz, Muhammad Taha, Ajmal Khan, Shahnaz Perveen, M. Iqbal Choudhary, Wolfgang Voelter,
Tópico(s)Click Chemistry and Applications
ResumoThiourea 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.
Referência(s)