Abstract
OBJECTIVE To study the design and synthesis of new territrem B analogues and their biological evaluation.METHODS New territrem B analogues 10a～10l with the common structure of 2H-pyran-2-one were designed and synthesized from ethyl acetoacetate.The cytotoxicities and inhibitory activities on acetylcholinesterase and butylcholinesterase of these synthetic analogues were examined by MTT and ELISA methods,respectively.RESULTS New analogues of territrem B were afforded and the structures were confirmed by 1H-NMR,ESI-MS and IR spectra.Compound 10f showed IC50 value to acetylcholinesterase at 6.98×10-5 mol·L-1 and all target compounds showed no inhibition to butylcholinesterase at 4.0 g·L-1.CONCLUSION The bioassay results indicated that 10f exhibited potential AChE inhibitory effect and better selectivity of AChE.
Key words
new territrem B analogues /
2H-pyran-2-one /
acetylcholinesterase inhibitor /
synthesis
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O Lei;JING Xing-rui;LI Dong-sheng;DONG Sheng-yi;OU YNG Ying-hu;I Hu;ZHO Yu.
Studies on Synthesis of New Territrem B Analogues and Their Biological Activities [J]. Chinese Pharmaceutical Journal, 2006, 41(18): 1423-1427
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