| Title : Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy - Li_2014_Bioorg.Med.Chem_22_4717 |
| Author(s) : Li Y , Peng P , Tang L , Hu Y , Sheng R |
| Ref : Bioorganic & Medicinal Chemistry , 22 :4717 , 2014 |
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Abstract :
A series of novel 2-methoxy-phenyl dimethyl-carbamate derivatives were designed, synthesized and evaluated as site-activated MTDLs based on rivastigmine and curcumin. Most of them exhibited good to excellent AChE and BuChE inhibitory activities with sub-micromolar IC50 values. Among all the compounds, 6a demonstrated the most potent AChE inhibition with IC50 value of 0.097microM, which is about 20-fold than that of rivastigmine. In addition, the three selected compounds 5a, 6a and 6e demonstrated inhibitory activity against Abeta self-aggregation similar to cucurmin in TEM assay, which is obviously different from the weak activity of rivastigmine. Moreover, the hydrolysate of 6a (compound 7) also showed potent ABTS(+) scavenging and moderate copper ion chelating activity in vitro. |
| PubMedSearch : Li_2014_Bioorg.Med.Chem_22_4717 |
| PubMedID: 25082512 |
Li Y, Peng P, Tang L, Hu Y, Sheng R (2014)
Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy
Bioorganic & Medicinal Chemistry
22 :4717
Li Y, Peng P, Tang L, Hu Y, Sheng R (2014)
Bioorganic & Medicinal Chemistry
22 :4717