| Summary: | In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as alpha-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by (HNMR)-H-1, (CNMR)-C-13, and EI-MS, and evaluated for alpha-amylase inhibition. Except compound 11 all analogs showed alpha-amylase inhibitory activity with IC50 values from 1.709 +/- 0.12 to 3.049 +/- 0.25 mu M against the standard acarbose (IC50 = 1.637 +/- 0.153 mu M). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 +/- 0.03, 1.747 +/- 0.20, 1.709 +/- 0.12, and 1.948 +/- 0.23 mu M, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done.
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