Title:Antiglycation Activity of N, N-Diethylthiobarbiturates Derivatives
Volume: 17
Issue: 4
Author(s): Momin Khan*, Ghulam Ahad, Ajmal Khan, Sana Shah, Kanwal, Uzma Salar, Syed Muhammad Salman and Khalid Mohammed Khan*
Affiliation:
- Department of Chemistry, Abdul Wali Khan University, Mardan 23200,Pakistan
- H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270,Pakistan
Keywords:
N, N-Diethylthiobarbiturates, antiglycation, aromatic aldehydes, dual inhibitor, rutin, α-glucosidase inhibitor.
Abstract:
Background: Previous identification of N,N-diethylthiobarbiturates as potential
α-glucosidase inhibitory potential prompted us to investigate the antiglycation activity of these
synthetic compounds (1-25) in order to identify the lead candidates for their possible antidiabetic
potential.
Methods: Synthetic compounds (1-25) were evaluated for their antiglycation activity using Bovine
Serum Albumin assay (BSA).
Result: Compounds exhibited varying degree of inhibition in the range of IC50 = 61.16 ± 2.3 - 656.71
± 2.5 µM as compared to the standard rutin (IC50 = 294.5 ± 1.50 µM). Among the twenty five
synthetic molecules, seven compounds showed good activity in comparison with the standard.
Compound 4 (IC50 = 61.16 ± 2.3 µM) having hydroxy substituents was the most active molecule of
the library. This study revealed that compound 4 has dual acting antidibetic molecule.
Conclusion: In conclusion, the synthetic N,N-diethylthiobarbiturates can act as lead molecules.
Furthermore, synthetic variations on N,N-diethylthiobarbituric acid moiety might be helpful in
generating a library of potential anti diabetic agent. Especially, compound 4 has been identified as
dual acting antidiabetic agent i.e. α-glucosidase inhibitor and antiglycating agent.
