Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study

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Abstract

Piperazine Sulfonamide analogs (1–19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1–19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.

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Taha, M., Irshad, M., Imran, S., Chigurupati, S., Selvaraj, M., Rahim, F., … Khan, K. M. (2017). Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study. European Journal of Medicinal Chemistry, 141, 530–537. https://doi.org/10.1016/j.ejmech.2017.10.028

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