Inhibition studies of Helicobacter pylori urease with Schiff base copper(ii) complexes

Abstract

Nine new copper(ii) complexes derived from various Schiff bases were prepared. Five complexes show effective urease inhibitory activities. Complex5has the most effective activity against urease, with a mixed competitive inhibition mechanism.

Symmetrical Heterocyclic Cage Skeleton: Synthesis, Urease Inhibition Activity, Kinetic Mechanistic Insight, and Molecular Docking Analyses

“…The development of competitive and non-competitive enzyme inhibitors based on a metalloskeleton has attracted wide interest of the scientific community because metal ions are found in the active sites of a large number of metalloproteins, such as hemocyanin, and also in metalloenzymes, like ureases, tyrosinase, laccase, and ascorbate oxidase [1,2,3,4,5,6,7,8]. The enzyme inhibition by the metallocompouds is due to the reaction of the organic skeleton as well as the transition metal ions with the sulfhydryl group in the active center of the enzyme [9].…”

Fabrication of metal–organic salts with heterogeneous conformations of a ligand as dual-functional urease and nitrification inhibitors

“…As a comparison, acetohydroxamic acid (AHA) was further used as a reference drug with a percent inhibition of 84.30%, and an IC 50 value of 37.2 ± 4.0 μM. 31 In addition, Cu 2+ can inhibit urease activity with an IC 50 value of 8.8 ± 1.4 μM. 32 Based on the above comparison, MOS 1 has a stronger activity than the metal salt, ligands and other MOSs, which may be attributed to Cu 2+ with higher urease inhibitory activity and its N-donor ligand with a synergistic effect.…”

Schiff bases and their metal complexes as urease inhibitors – A brief review

“…Complex 36 ( Fig. 6 ), which had the best anti-urease activity (IC 50 = 0.03 µM), was shown to be a mixed-competitive inhibitor ( K i = 15.0 µM) [41] . Pervez and co-workers (2016) also synthesized some copper complexes of isatin-derived bis -Schiff base ligands, and they evaluated the anti-urease activities of all synthesized complexes.…”