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CAN catalyzed one-pot synthesis of Imidazole derivatives in PEG-400 as HMG-CoA reductase inhibitor for benefit in atherosclerosis

Zong-Sheng Guo, Xin-Chun Yang

Aim: The present study was intended to develop some novel imidazole derivatives via multi-component reaction catalysed by Ceric Ammonium Nitrate (CAN) in polyethylene glycol-400 (PEG-400) and its HMG-CoA reductase inhibitory activity for benefit in atherosclerosis.

Methods: The one-pot synthesis has been achieved by taking benzyl, benzaldehyde, 3-amino-1, 2, 4- triazole-5- carboxylic acid (0.01 mol) in PEG-400 with CAN as a catalyst. These derivatives were subjected for anti-oxidant activity using DPPH free radical scavenging assay, together with determination of inhibitory activity against HMG-CoA reductase.

Results: Among the tested compounds, compound 4i was identified as most promising compound exhibiting considerable quenching activity with IC₅₀=3.1 ± 0.7 μM in DPPH assay. The compounds were further screened for HMG-CoA reductase inhibitory activity, where few analogues found to exhibit potent activity.

Conclusion: All target derivatives have may exert beneficial effect in atherosclerosis via inhibition of HMG-CoA reductase together with anti-oxidant activity.