| Title : Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids - Huang_2012_Bioorg.Med.Chem_20_3038 |
| Author(s) : Huang L , Su T , Shan W , Luo Z , Sun Y , He F , Li X |
| Ref : Bioorganic & Medicinal Chemistry , 20 :3038 , 2012 |
|
Abstract :
A series of berberine-phenyl-benzoheterocyclic (26-29) and tacrine-phenyl-benzoheterocyclic hybrids (44-46) were synthesised and evaluated as multifunctional anti-Alzheimer's disease agents. Compound 44b, tacrine linked with phenyl-benzothiazole by 3-carbon spacers, was the most potent AChE inhibitor with an IC(50) value of 0.017 muM. This compound demonstrated similar Abeta aggregation inhibitory activity with cucurmin (51.8% vs 52.1% at 20 muM, respectively), indicating that this hybrid is an excellent multifunctional drug candidate for AD. |
| PubMedSearch : Huang_2012_Bioorg.Med.Chem_20_3038 |
| PubMedID: 22472046 |
| Inhibitor | Berberine |
Huang L, Su T, Shan W, Luo Z, Sun Y, He F, Li X (2012)
Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids
Bioorganic & Medicinal Chemistry
20 :3038
Huang L, Su T, Shan W, Luo Z, Sun Y, He F, Li X (2012)
Bioorganic & Medicinal Chemistry
20 :3038