Synthesis of andrographolide derivatives: a new family of alpha-glucosidase inhibitors |
| |
Authors: | Xu Hai-Wei Dai Gui-Fu Liu Gai-Zhi Wang Jun-Feng Liu Hong-Min |
| |
Institution: | New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450052, PR China. |
| |
Abstract: | Andrographolide (1), the cytotoxic agent of the plant Andrographis paniculata, was subjected to semi-synthetic studies leading to a series of new derivatives, a novel family of glucosidase inhibitors. Nicotination of 3,19-hydroxyls in 15-alkylidene andrographolide derivatives (9) was favorable to alpha-glucosidase inhibition activity. Among them, 15-p-chlorobenzylidene-14-deoxy-11,12-didehydro-3,19-dinicotinateandrographolide (11c) was a very potent inhibitor against alpha-glucosidase with an IC50 value of 6 microM. However, all compounds concerned for beta-glucosidase showed no inhibition. All compounds synthesized were characterized by the analysis of NMR, IR, HRMS spectra and the stereochemistry of 2 was confirmed by X-ray analysis. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|