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
Highlights
The worldwide increase in gastro-intestinal diseases, i.e. peptic ulcers, kidney stones, urinary tract infections and hepatic coma often lead to the worst cases of liver cirrhosis and kidney cancers [1, 2]
A nickel containing metallo-enzyme, catalyzes the hydrolysis of urea into ammonia and carbamic acid which spontaneously decompose to yield a second molecule of ammonia and carbon dioxide resulting of elevation in pH and enabling H. pylori to survive in the extreme acidic conditions of stomach [5,6,7,8]
In order to investigate the influence of N,S,O-mixed ligands on the urease inhibitory behavior, four Nsubstituted R-phenylethanamine derivatives have been selected
Summary
The worldwide increase in gastro-intestinal diseases, i.e. peptic ulcers, kidney stones, urinary tract infections and hepatic coma often lead to the worst cases of liver cirrhosis and kidney cancers [1, 2]. [LBZnCl2] was prepared according to the similar procedure described for [LAZnCl2] except utilizing LB (1.06 g, 4.60 mmol) to yield white precipitate (1.50 g, 88%); mp 171 °C; FTIR (solid neat; cm-1): ν(N‐H) 3267 w; ν(C‐H) 2951 w; ν(C=C) 1636 s; (‐C‐H sp3) 1455 m; ν(N-C) 1308 w; (C-H sp2) 873 m;ν(C-S) 850 m; ν(M-N) 558 s; 1H NMR (CDCl3, 400 MHz): δ = 7.907.80 (2H, m, ArH), 7.40 (3H, m, ArH), 6.77 (1H, m, ArH), 6.52 (1H, m, ArH), 4.48
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
