Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374441 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
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.
Graphical abstractA 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 full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David G. Washburn, Tram H. Hoang, Nino Campobasso, Angela Smallwood, Derek J. Parks, Christine L. Webb, Kelly A. Frank, Melanie Nord, Chaya Duraiswami, Christopher Evans, Michael Jaye, Scott K. Thompson,