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Paper | Regular issue | Vol 92, No. 8, 2016, pp.1430-1439
Published online, 20th June, 2016
DOI: 10.3987/COM-16-13491
One-Pot and Three-Component Synthesis, Characterization and Biological Evaluation of Some New 1,2,4-Triazine-coumarins

Guang-cheng Wang,* Jing Wang, Dian-xiong He, Xin Li, Juan Li, and Zhi-yun Peng

*College of Chemistry and Chemical Engineering, Jishou University, Jishou University, Jishou 416000, China

Abstract

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 1H NMR, 13C NMR and melting points. Furthermore, all newly synthesized compounds were evaluated for their α-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 μM, when compared to the standard acarbose (IC50 = 876.14±2.46 μM).