Exploring thiazole-based Schiff base analogs as potent α-glucosidase and α-amylase inhibitor: their synthesis and in-silico study
Journal of Molecular Structure(2023)
摘要
In search of potent antidiabetic agents here in this study a new series of thiazole-based Schiff base analogs (1–20) have been synthesized, characterized by 1HNMR, 13CNMR, HREI-MS and evaluated as dual inhibitor for α-glucosidase and α-amylase. All analogs of the series found active and exhibited variable degree of inhibitory potential ranging from 1.10 ± 0.10–17.20 ± 0.30 µM as compared to reference drug acarbose IC50 = for 9.80 ± 0.20 µM α-glucosidase and from 0.90 ± 0.01 to 16.20 ± 0.30 µM as compared to reference drug acarbose IC50 = 10 0.30 ± 0.20 µM for α-amylase. Compounds 3, 5, 6, 7, 14, 15, 16, 18 and 19 exhibited outstanding α-glucosidase as well as α-amylase inhibitory potential as compared to reference drug acarbose. Structure activity relationships SAR) have established for all the synthesized analogs. A molecular docking study has been conducted to develop an idea about binding interaction of compounds and enzymes. All synthesized compounds were tested for cytotoxicity and found nontoxic.
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关键词
Thiazole,Α-glucosidase,Α-amylase,Schiff base,Structure activity relationship,Docking study
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