Antiglycation Activity of N, N-Diethylthiobarbiturates Derivatives

Background: Previous identification of N,N-diethylthiobarbiturates as potential alpha-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 mu M as compared to the standard rutin (IC50 = 294.5 +/- 1.50 mu M). Among the twenty five synthetic molecules, seven compounds showed good activity in comparison with the standard. Compound 4 (IC50 = 61.16 +/- 2.3 mu M) 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. alpha-glucosidase inhibitor and antiglycating agent.