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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 Nizwa, P.O. Box 33, Birkat 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, H .E. J. Research Institute of Chemistry, 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



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