cinnamoyl-chloride and Alzheimer-Disease

To develop of new class of selective and reversible MAO-B inhibitors from enamides.. Syntheses of the titled derivatives (AD1-AD11) were achieved by reacting cinnamoyl chloride and various primary and secondary amines in basic medium. All eleven compounds were investigated for in vitro inhibitory activities against recombinant human MAO-A and MAO-B. The reversibilities of lead compound inhibitions were analysed by dialysis. MTT assays of lead compounds were performed using normal VERO cell lines.. These results encourage further studies on the enamide scaffold as potential drug candidates for the treatment of Alzheimer's and Parkinson's diseases.

Topics: Alzheimer Disease; Amines; Binding, Competitive; Cinnamates; Drug Design; Drug Discovery; Humans; Hydrogen Bonding; Molecular Docking Simulation; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Parkinson Disease; Structure-Activity Relationship