Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors

Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders.

Graphical abstractUsing structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase inhibitors were discovered.Figure optionsDownload full-size imageDownload as PowerPoint slide