ONE-POT AND THREE-COMPONENT SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NEW 1,2,4-TRIAZINE-COUMARINS

被引：14

作者：

Wang, Guang-cheng ^{[1
]}

Wang, Jing ^{[1
]}

He, Dian-xiong ^{[1
]}

Li, Xin ^{[1
]}

Li, Juan ^{[1
]}

Peng, Zhi-yun ^{[1
]}

机构：

[1] Jishou Univ, Coll Chem & Chem Engn, Jishou 416000, Peoples R China

来源：

HETEROCYCLES | 2016年 / 92卷 / 08期

关键词：

GLUCOSIDASE INHIBITORY-ACTIVITY; ALPHA-GLUCOSIDASE; MOLECULAR DOCKING; DERIVATIVES; CHEMISTRY; COUMARINS; DESIGN; ANALOGS; LAMOTRIGINE; OBESITY;

D O I：

10.3987/COM-16-13491

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of 1,2,4-triazine-coumarins were prepared by a one-pot, three-component condensation of 1,2-diarylethane-1,2-diones, thiosemicarbazide and 2-coumaryloxy-methyloxiranes using K2CO3 as a catalyst in aqueous medium. This three-component reaction offers several advantages such as simple procedure, environmentally friendly and high yields. The resulting products were characterized by H-1 NMR, C-13 NMR, HRMS and melting points. Furthermore, all newly synthesized compounds were evaluated for their a-glucosidase inhibitory activity. As a result, the majority of the screened compounds displayed potent inhibitory activity with IC50 values in the range of 32.57+/-0.21 to 148.77+/-3.23 mu M, when compared to the standard acarbose (IC50 = 876.14+/-2.46 mu M)

引用

页码：1430 / 1439

页数：10

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