Paper Report for: Mao_2013_Bioorg.Med.Chem.Lett_23_6737
Reference
Title: Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity Mao F, Chen J, Zhou Q, Luo Z, Huang L, Li X Ref: Bioorganic & Medicinal Chemistry Lett, 23:6737, 2013 : PubMed
A series of tacrine-ebselen hybrids were synthesised and evaluated as possible multifunctional anti-Alzheimer's disease (AD) agents. Compound 6i, which is tacrine linked with 5,6-dimethoxybenzo[d][1,2]selenazol-3(2H)-one by a six-carbon spacer, was the most potent acetylcholinesterase (AChE) and butylcholinesterase (BCHE) inhibitor, with IC50 values of 2.55 and 2.80nM, respectively. Furthermore, this compound demonstrated similar hydrogen peroxide and peroxynitrite scavenging activity as ebselen by horseradish peroxidase assay and peroxynitrite scavenging activity assay, indicating that this hybrid is a good multifunctional drug candidate for the treatment of AD.
Mao F, Chen J, Zhou Q, Luo Z, Huang L, Li X (2013) Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity Bioorganic & Medicinal Chemistry Lett23: 6737-42
Mao F, Chen J, Zhou Q, Luo Z, Huang L, Li X (2013) Bioorganic & Medicinal Chemistry Lett23: 6737-42