Background: Due to high demand of developing new compounds to solve the health
issues, paracetamol resembling 4-acetamidobenzaldehyde was derivatized into different new compounds
including important pharmacophores (benzimidazole, benzothiazole). The synthesized
compounds were investigated for anti-Alzheimer, antioxidant and DNA binding abilities.
Methods: The new compounds were synthesized by the well-established synthetic routes. All synthesized
compounds were analysed by H-NMR, 13C-NMR, Mass spectrometry and FTIR. Spectrophotometric
method was applied for determination of inhibition potency against AChE and BChE.
DPPH free radical scavenging method was used to check the antioxidant ability and the spectrophotometric
titration was utilized to study the binding ability of synthesized derivatives with DNA.
Results: 4-Acetamdiobenzaldehyde based derivatives were synthesized and characterised by HNMR,
13C-NMR, Mass spectrometry and FTIR. The synthesized compounds were analysed for
anti-Alzheimer activity and results were compared by docking showed that 18 and 2 are good inhibitors
of AChE and BChE. The results of DPPH radical scavenging activity explored most of the
synthesized compounds as good antioxidants, out of these 18 showed maximum scavenging activities.
Furthermore, compound 2 exhibited maximum intrinsic binding constant (K= 9.64×105M-1)
Conclusion: A new series of 4-Acetamidobenzaldehyde derivatives (1-20) were synthesized,
characterized and studied for their antioxidant, anti-Alzheimer and DNA binding abilities. The results
of anti-Alzheimer activity were compared by docking. Most of the synthesized compounds
showed very significant antioxidants, anti-cholinesterase activities. All the compounds showed
weak interaction with the DNA. These compounds are suitable for further pharmacological investigations.