Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372887 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Balancing potency and metabolic stability in a target which favours lipophilic ligands is a considerable challenge. Here we describe two strategies employed to achieve this balance in a series of pyrazolopyrimidine CRF antagonists: moderation of lipophilicity, and incorporation of a metabolically stable lipophilic group.
Graphical abstractBalancing potency and metabolic stability in a target which favours lipophilic ligands is a considerable challenge. Here we describe two strategies employed to achieve this balance in a series of pyrazolopyrimidine CRF antagonists: moderation of lipophilicity, and incorporation of a metabolically stable lipophilic group.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Duncan C. Miller, Wolfgang Klute, Andrew Calabrese, Alan D. Brown,