Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRα will be disclosed.

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. This manuscript will describe optimization of this series of LXR agonists using a structure-based design strategy. In addition, the SAR of this novel series and a crystal structure of a selected ligand bound to the LXRα LBD will be disclosed.Figure optionsDownload as PowerPoint slide