Synthesis, characterization and urease inhibitory activities of Zn(II) complexes bearing C1-symmetric ligands derived from (R)-phenylethanamine

Abstract

ABSTRACT. A series of Zn(II) complexes, supported with N-substituted phenylethanamine derivatives, [LnZnCl2] (where Ln = LA ((R)-1-phenyl-N-(thiophene-2-ylmethyl)ethanamine; LB (R)-N-(5-meyhylthiophene-2-yl)methyl-1-phenylethanamine; LC ((R)-N-(furan-2-ylmeththyl)-1-phenylethanamine and LD (R)-N-((5-methylfuran-2-yl)methyl)-1-phenylethanamine) were synthesized and characterized. The urease inhibitory activities of these complexes were determined against selected urease inhibitors where [LBZnCl2] was found to be the most prominent inhibitor of Jack bean urease (J. B. urease) (IC50 = 10.39±0.78 μM), whereas the activity of Bacillus pasteurii urease (B. P. urease) was predominantly inhibited by [LAZnCl2] (IC50 = 8.68±0.7 μM). Additionally, MOE-Dock program was used to affirm the probable binding modes of these complexes into the crystal structure of J. B. urease which certainly verified the inhibitory mechanism of these novel complexes.                     KEY WORDS: Zn(II) complexes, (R)-Phenylethanamine, Urease inhibition, Molecular docking   Bull. Chem. Soc. Ethiop. 2021, 35(2), 301-314. DOI: https://dx.doi.org/10.4314/bcse.v35i2.7