Design, Synthesis, and Biological Evaluation of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Acetylcholinesterase Inhibitors

作者：Liu, Si-Jie; Yang, Liu; Liu, Xiao-Guang; Luo, Ying; Cao, Zi-Jian; Wan, David Chi Cheong; Lin, Huang-Quan; Hu, Chun^*

来源：Letters in Drug Design and Discovery, 2010, 7(1): 5-8.

DOI：10.2174/157018010789869343

• Acetylcholinesterase
• Inhibitors
• Synthesis
• Heterocycles
• Docking
• 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivative

The docking study on a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives with acetylcholinesterase has been demonstrated. The synthesis and characterization of a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were described. All target compounds were evaluated in vitro for the inhibitory activities against AChE via Ellman colorimetric assay. Most of the target compounds possessed anti-acetylcholinesterase activity. The preliminary structure-activity relationships were discussed.

• 单位
  香港中文大学; 沈阳药科大学