A series of naphthalene ring containing 2,4,5-trisubstituted imidazole derivatives (2a–2l) were synthesized using one-pot multicomponent reaction. The reactions were carried out using naphthaldehyde and substituted benzil in the presence of ammonium acetate in acetic acid media. All newly synthesized imidazole derivatives were characterized by FT-IR, 1H NMR, 13C NMR and mass spectral analysis. Newly synthesized imidazole derivatives were screened for their in-vitro antioxidant activity by DPPH free radical scavenging assay method and α-amylase inhibition activity by DNS method. All the compounds showed excellent α-amylase activity at 10, 50 and 100 μg/mL and compounds 2d, 2g, 2k exhibited good antioxidant activity.
