Exploring thiazole-based Schiff base analogs as potent -glucosidase and -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 alpha-glucosidase and alpha-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 mu M as compared to reference drug acarbose IC50 = for 9.80 +/- 0.20 mu M alpha-glucosidase and from 0.90 +/- 0.01 to 16.20 +/- 0.30 mu M as compared to reference drug acarbose IC50 = 10 0.30 +/- 0.20 mu M for alpha-amylase. Compounds 3, 5, 6, 7, 14, 15, 16, 18 and 19 exhibited outstanding alpha-gluco-sidase as well as alpha-amylase inhibitory potential as compared to reference drug acarbose. Structure activity re-lationships 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, A-glucosidase, A-amylase, Schiff base, Structure activity relationship, Docking study
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