Muhammad Jamil,
Nargis Sultana,
Rizwan Ashraf,
Muhammad Sarfraz,
Muhammad Ilyas Tariq 
,
Muhammad Mustaqeem
For correspondence:- Muhammad Tariq Email: tariqmi@uos.edu.pk
Accepted: 24 February 2018 Published: 31 March 2018
Citation: Jamil M, Sultana N, Ashraf R, Sarfraz M, Tariq MI, Mustaqeem M. Tris-diamine-derived transition metal complexes of flurbiprofen as cholinesterase inhibitors. Trop J Pharm Res 2018; 17(3):451-459 doi: 10.4314/tjpr.v17i3.10
© 2018 The authors.
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 Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
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
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