Paper Report for: Huang_2014_Eur.J.Med.Chem_81C_15
Reference
Title: Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine Huang G, Kling B, Darras FH, Heilmann J, Decker M Ref: Eur Journal of Medicinal Chemistry, 81C:15, 2014 : PubMed
Two sets of carbamates based on the natural alkaloid evodiamine were designed, synthesized and evaluated as potential butyrylcholinesterase inhibitors. Although a set of carbamates of 3-hydroxyevodiamine (10a-f) is inactive both at AChE and BChE, carbamates of 5-deoxo-3-hydroxyevodiamine (11a-f) exhibit much better potency with selectivity toward BChE. The heptyl carbamate of 5-deoxo-3-hydroxyevodiamine (11c) shows the best potency with an IC50 value of 77 nM and very good selectivity over AChE. ORAC and cell-based assays indicate 11c owns pronounced antioxidant properties with 1.75 Trolox equivalents and strong neuroprotection even from 1 muM onwards. These combined activities might enable compound 11c to be a potential candidate for treatment of Alzheimer's disease.
Huang G, Kling B, Darras FH, Heilmann J, Decker M (2014) Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine Eur Journal of Medicinal Chemistry81C: 15-21
Huang G, Kling B, Darras FH, Heilmann J, Decker M (2014) Eur Journal of Medicinal Chemistry81C: 15-21
