| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376770 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
The structure–activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagoinsts (e.g., 2–5) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pattern of the pyridine ring. A stereoselective intramolecular Michael addition reaction to the vinyl pyridine group was observed for these pyridine analogs of himbacine in basic conditions at elevated temperature.
Graphical abstractThe structure–activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagoinsts is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yan Xia, Samuel Chackalamannil, Tze-Ming Chan, Michael Czarniecki, Darío Doller, Keith Eagen, William J. Greenlee, Hsingan Tsai, Yuguang Wang, Ho-Sam Ahn, George C. Boykow, Andrew T. McPhail,