Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370348 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b as a highly potent MCH-R1 antagonist. This compound also has favorable pharmacokinetic properties along with a high metabolic stability and a minimal impact on CYP isoforms and hERG.
Graphical abstractThe synthesis and SAR of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as MCH-R1 antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chae Jo Lim, Ji Young Kim, Byung Ho Lee, Kwang-Seok Oh, Kyu Yang Yi,