| Title : Synthesis and biological evaluation of functionalized coumarins as acetylcholinesterase inhibitors - Shen_2005_Eur.J.Med.Chem_40_1307 |
| Author(s) : Shen Q , Peng Q , Shao J , Liu X , Huang Z , Pu X , Ma L , Li YM , Chan AS , Gu L |
| Ref : Eur Journal of Medicinal Chemistry , 40 :1307 , 2005 |
|
Abstract :
Three series of functionalized coumarin compounds were designed and prepared as cholinesterase (AChE and BuChE) inhibitors. The biological profile against AChE and BuChE of the prepared compounds was determined. Compound 7b exhibited a mixed-type of AChE inhibitor with IC50 value for the AChE inhibition of 0.19+/-0.01 microM and a high selectivity for AChE/BuChE, and compound 6b acted as non-competitive AChE inhibitor with IC50 value of 0.43+/-0.02 microM. Structure-activity relationships (SARs) of prepared compounds were discussed. |
| PubMedSearch : Shen_2005_Eur.J.Med.Chem_40_1307 |
| PubMedID: 16182411 |
Shen Q, Peng Q, Shao J, Liu X, Huang Z, Pu X, Ma L, Li YM, Chan AS, Gu L (2005)
Synthesis and biological evaluation of functionalized coumarins as acetylcholinesterase inhibitors
Eur Journal of Medicinal Chemistry
40 :1307
Shen Q, Peng Q, Shao J, Liu X, Huang Z, Pu X, Ma L, Li YM, Chan AS, Gu L (2005)
Eur Journal of Medicinal Chemistry
40 :1307