| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10595327 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A novel series of piperazine derivatives exhibits sub-nanomolar binding and enhanced subtype selectivity as δ-opioid agonists. The synthesis and SAR are described as well as the application of computational models to improve in vitro ADME and safety properties suitable for CNS indications, specifically microsomal clearance, permeability, and hERG channel inhibition.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John P. Jr., Cathy L. Dantzman, Megan M. King, Glen E. Ernst, Xia Wang, Kelly Brush, William E. Palmer, William Frietze, Donald W. Andisik, Valerie Hoesch, Kenneth Doring, James Hulsizer, Khanh H. Bui, Jay Liu, Thomas J. Hudzik, Steven S. Wesolowski,