Title : Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease - Luo_2014_Bioorg.Med.Chem_22_1355 |
Author(s) : Luo Z , Liang L , Sheng J , Pang Y , Li J , Huang L , Li X |
Ref : Bioorganic & Medicinal Chemistry , 22 :1355 , 2014 |
Abstract :
A series of ebselen derivatives were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and glutathione peroxidase (GPx) mimics. Most of the compounds were found to be potent against AChEs and BCHE, compounds 5e and 5i, proved to be the most potent against AChE with IC(5)(0) values of 0.76 and 0.46 muM, respectively. Among these hybrids, most of the compounds were found to be good GPx mimics compare with ebselen. The selected compounds 5e and 5i were also used to determine the catalytic parameters and in vitro hydrogen peroxide scavenging activity. The results indicate that compounds 5e and 5i may be excellent multifunctional agents for the treatment of AD. |
PubMedSearch : Luo_2014_Bioorg.Med.Chem_22_1355 |
PubMedID: 24461494 |
Inhibitor | Ebselen |
Luo Z, Liang L, Sheng J, Pang Y, Li J, Huang L, Li X (2014)
Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease
Bioorganic & Medicinal Chemistry
22 :1355
Luo Z, Liang L, Sheng J, Pang Y, Li J, Huang L, Li X (2014)
Bioorganic & Medicinal Chemistry
22 :1355