Submit Manuscript  

Article Details


Antiglycation Activity of N, N-Diethylthiobarbiturates Derivatives

[ Vol. 17 , Issue. 4 ]

Author(s):

Momin Khan*, Ghulam Ahad, Ajmal Khan, Sana Shah, Kanwal, Uzma Salar, Syed Muhammad Salman and Khalid Mohammed Khan*   Pages 411 - 417 ( 7 )

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.

Keywords:

N, N-Diethylthiobarbiturates, antiglycation, aromatic aldehydes, dual inhibitor, rutin, α-glucosidase inhibitor.

Affiliation:

Department of Chemistry, Abdul Wali Khan University, Mardan 23200, Department of Chemistry, Abdul Wali Khan University, Mardan 23200, Natural and Medical Sciences Research Center, University of NizwaBirkat Al Mauz, Nizwa 616, Department of Chemistry, Abdul Wali Khan University, Mardan 23200, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Department of Chemistry, Islamia College University Peshawar, Peshawar 25120, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270

Graphical Abstract:



Read Full-Text article