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一系列新型席夫碱衍生物含 1,2,3-三唑:设计、合成、分子对接和α-葡萄糖苷酶抑制作用。

A new series of Schiff base derivatives bearing 1,2,3-triazole: Design, synthesis, molecular docking, and α-glucosidase inhibition.

机构信息

Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.

Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.

出版信息

Arch Pharm (Weinheim). 2019 Aug;352(8):e1900034. doi: 10.1002/ardp.201900034. Epub 2019 Jul 22.

Abstract

A series of new Schiff bases bearing 1,2,3-triazole 12a-o was designed, synthesized, and evaluated as α-glucosidase inhibitors. All the synthesized compounds showed promising inhibition against α-glucosidase and were more potent than the standard drug acarbose. The kinetic study on the most potent compound 12n showed that this compound acted as a competitive α-glucosidase inhibitor. The docking study revealed that the synthesized compounds interacted with the important residues in the active site of α-glucosidase.

摘要

设计、合成并评价了一系列新型含 1,2,3-三唑的 Schiff 碱 12a-o,作为α-葡萄糖苷酶抑制剂。所有合成的化合物均表现出对α-葡萄糖苷酶的良好抑制作用,且比标准药物阿卡波糖更有效。对最有效的化合物 12n 的动力学研究表明,该化合物为竞争性α-葡萄糖苷酶抑制剂。对接研究表明,合成的化合物与α-葡萄糖苷酶活性部位的重要残基相互作用。

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