Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593387 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 receptor antagonists based on the benzazepine core. Employing an H3 driven pharmacodynamic model, the series was then further optimised through to a lead compound that showed robust in vivo functional activity and possessed overall excellent developability properties.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David M. Wilson, James Apps, Nicholas Bailey, Mark J. Bamford, Isabel J. Beresford, Michael A. Briggs, Andrew R. Calver, Barry Crook, Robert P. Davis, Susannah Davis, David K. Dean, Leanne Harris, Tom D. Heightman, Terry Panchal, Christopher A. Parr,