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, 2-diaminoethane-derived 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.Keywords: Flurbiprofen, Cholinesterase, Diamines, Galantamine, Metal complexes, Cholinesterase inhibition
Highlights
INTRODUCTIONPeople suffer from Alzheimer Disease (AD), and that this number is expected to quadruple in the
Tropical Journal of Pharmaceutical Research is indexed by Science Citation Index (SciSearch), Scopus, International Pharmaceutical Abstract, Chemical Abstracts, Embase, Index Copernicus, EBSCO, African Index Medicus, JournalSeek, Journal Citation Reports/Science Edition, Directory of Open Access Journals (DOAJ), African Journal Online, Bioline International, Open-J-Gate and Pharmacy Abstracts people suffer from Alzheimer Disease (AD), and that this number is expected to quadruple in the
To each stirred suspension of synthesized flurbiprofen metal complexes (3a-3c) in ethanol/water (1:1, v:v) solution, 1.68 ml of 1,3diaminopropane (0.02 mole) was added, and reaction mixtures were stirred for 15-20 min at room temperature until they became clear with characteristic colors of the metal complexes
Summary
People suffer from Alzheimer Disease (AD), and that this number is expected to quadruple in the. The reaction mixtures were stirred for 15-20 min at room temperature until they became clear with characteristic colors Slow evaporation of these solutions produced the desired solid products tris (1, 2-diaminopropane)-flurbiprofen metal complexes (4a-4c). To each stirred suspension of synthesized flurbiprofen metal complexes (3a-3c) in ethanol/water (1:1, v:v) solution, 1.68 ml of 1,3diaminopropane (0.02 mole) was added, and reaction mixtures were stirred for 15-20 min at room temperature until they became clear with characteristic colors of the metal complexes. Slow evaporation of these solutions produced the desired solid tris (1,3-diaminopropane)flurbiprofen metal complexes (5a-5c). Absorbance was read thrice at 412 nm, and IC50 values of the compounds were calculated by plotting sample concentration against inhibition
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