| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362194 | Bioorganic & Medicinal Chemistry Letters | 2011 | 8 Pages |
Abstract
To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.
Graphical abstractTo improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, GSK2324 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jonathan Y. Bass, Justin A. Caravella, Lihong Chen, Katrina L. Creech, David N. Deaton, Kevin P. Madauss, Harry B. Marr, Robert B. McFadyen, Aaron B. Miller, Wendy Y. Mills, Frank Navas III, Derek J. Parks, Terrence L. Smalley Jr., Paul K. Spearing,