Literature

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.

DOI： 10.1016/j.ejmech.2014.01.001

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

European Journal of Medicinal Chemistry 2014.0

Synthesis and structure–activity relationship of thiobarbituric acid derivatives as potent inhibitors of urease

Bioorganic & Medicinal Chemistry 2014.0

Design and synthesis of new barbituric- and thiobarbituric acid derivatives as potent urease inhibitors: Structure activity relationship and molecular modeling studies

Bioorganic & Medicinal Chemistry 2015.0

Bisindolylmethane thiosemicarbazides as potential inhibitors of urease: Synthesis and molecular modeling studies

Bioorganic & Medicinal Chemistry 2018.0

Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial and urease inhibitors

Medicinal Chemistry Research 2013.0

Solution-phase microwave assisted parallel synthesis, biological evaluation and in silico docking studies of N,N′-disubstituted thioureas derived from 3-chlorobenzoic acid