1-1-diphenyl-2-picrylhydrazyl and acetamide

On the basis of our previous work, a novel series of (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives were synthesized and evaluated as multifunctional ligands for the treatment of Alzheimer's disease (AD). Biological evaluations indicated that the derivatives can be used as anti-AD drugs that have multifunctional properties, inhibit the activity of butyrylcholinesterase (BuChE), inhibit neuroinflammation, have neuroprotective properties, and inhibit the self-aggregation of Aβ. Compound f9 showed good potency in BuChE inhibition (IC

Topics: Acetamides; Alzheimer Disease; Amyloid beta-Peptides; Antioxidants; Biphenyl Compounds; Butyrylcholinesterase; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Drug Design; Humans; Molecular Structure; Neuroprotective Agents; Oxadiazoles; Picrates; Protein Aggregates; Structure-Activity Relationship

In recent years, antioxidant compounds play an important role as a health-protecting factor. Antioxidants protect cells against the damaging effects of reactive oxygen species (ROS). An imbalance between antioxidants and ROS results in oxidative stress, which leads to cellular damage and it is linked to many vital diseases. It was shown that heme oxygenase (HO) provides efficient cytoprotection against oxidative stress. In this study, a series of indole-2-carboxamide and 3-acetamide derivatives was tested for in vitro effects on HO activity and 2,2-diphenyl-1-picrylhydrazyl (DPPH) inhibition. Among the synthesized compounds, N-[3-(dimethylamino)propyl]-1H-indole-2-carboxamide 3 was found as the most activator of HO and N-(2-(dimethylamino)ethyl)-2-(1H-indol-3-yl)acetamide 8 was found the most potent inhibitor for DPPH at 10(-4) M concentration.

Topics: Acetamides; Antioxidants; Biphenyl Compounds; Chemistry Techniques, Synthetic; Dose-Response Relationship, Drug; Heme Oxygenase (Decyclizing); Indoles; Picrates; Structure-Activity Relationship