Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors

This manuscript describes the design and synthesis of a series of pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. Analogs were optimized using structure-based design and physical property considerations resulting in the identification of 44, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and chronic efficacy in a pre-clinical animal models.

Graphical abstractThis manuscript describes the design and synthesis of a series of N-iso-propyl pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia.Figure optionsDownload full-size imageDownload as PowerPoint slide