Tris-diamine-derived transition metal complexes of flurbiprofen as cholinesterase inhibitors

Abstract

Purpose:To synthesize novel tris-diamine-derived transition metal complexes of flurbiprofen M(C2H8N2)3 (fp)2 and M(C3H10N2)3 (fp)2, and to evaluate their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Method: Tris-diamine-derived transition metal complexes of Co(II), Ni(II), and Mn(II) were synthesized and characterized using ultraviolet-visible (UV-Vis) spectroscopy, Fourier transform-infrared (FT-IR) spectroscopy, elemental analysis, magnetic susceptibility, conductivity measurement and single crystal x-ray analysis. The synthesized complexes were also evaluated for their AChE and BChE inhibitory activities. Results: Based on magnetic susceptibility and electronic studies, the synthesized complexes possessed distorted octahedral geometry. Conductance measurements indicated that diamine-derived metal complexes of flurbiprofen were electrolytes, whereas, simple metal complexes of flurbiprofen were non-electrolytes. The structure of Ni (C2H8N2)3 (fp)2 was also confirmed by single crystal x-ray analysis. The synthesized metal complexes exhibited moderate-to-very good inhibition of AChE and BChE. In vitro assays revealed that Ni complexes were most active, with the least half-maximal inhibitory concentration (IC50) values against AChE and BChE, compared to Co and Mn complexes. Furthermore,1, complexes were more potent, with lower IC50 values against both AChE and BChE, compared to 1,3-diaminopropane-derived complexes. Among the complexes, 4a and 5a revealed significant cholinesterase inhibitory activities relative to the standard drug, galantamine. Conclusion: All the synthesized metal complexes are active against AChE and BChE, but only 4a and 5a are more active than the standard drug, galantamine, indicating their potential for drug development. This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest

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“…12. Few Schiff bases used for complexation with metals by You et al [124,125] The Schiff base manganese complexes exhibit catalytic activity [126][127][128][129] and form polymeric structure through thiocyanato ligand. Recent studies indicated that Cu(II), Cd(II), Co(II,III) and Ni(II) complexes with Schiff base ligands display urease inhibitor activity.…”

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“…These results showed that the metal ions and ligands played an important role in urease inhibition. Besides, complex 40 with Mn (III) ions was synthesised 73 . However, the results of urease inhibition displayed that compound 40 (IC 50 = 61.05 μM) showed moderate urease inhibition on this enzyme as compared with thiourea, which was tested as the reference standard with an IC 50 value of 21.25 μM ( Figure 11 ).…”