Design, Synthesis and Biological Evaluation of Some 2‐Azetidinone Derivatives as Potential Antihyperlipidemic Agents

Abstract

In an effort to develop new molecules with improved antihyperlipidemic activity, eight new 2‐azetidinone analogs (4a–4h) of ezetimibe were designed through in silico docking experiments with the crystal structure of the Niemann‐Pick C1‐like 1 protein (NPC1L1). Synthesis and further antihyperlipdemic evaluation of this series in the Triton WR 1339 induced hyperlipidemic rat model showed some of the molecules to exhibit significant lipid‐lowering effects comparable to ezetimibe. Correlation between the observed biological activity and the in silico molecular docking scores of the compounds was observed.