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Letters in Drug Design & Discovery

Author(s): Momin Khan*, Ghulam Ahad, Ajmal Khan, Sana Shah, Kanwal, Uzma Salar, Syed Muhammad Salman and Khalid Mohammed Khan*

DOI: 10.2174/1570180816666190516111516

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Antiglycation Activity of N, N-Diethylthiobarbiturates Derivatives

Page: [411 - 417] Pages: 7

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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.

Graphical Abstract

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