Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376843 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
The synthesis and SAR for a novel series of 2-alkyl-4-aryl-tetrahydro-pyrido-pyrimidines and 2-alkyl-4-aryl-tetrahydro-pyrimido-azepines is described. Representative compounds were shown to be subtype selective 5-HT2A antagonists. Optimal placement of a basic nitrogen relative to the pyrimidine and the presence of a 4-fluorophenyl group in the pyrimidine 4-position was found to have a profound effect on affinity and selectivity.
Graphical abstractThe synthesis and SAR for a novel series of 2-alkyl-4-aryl-tetrahydro-pyrido-pyrimidines and 2-alkyl-4-aryl-tetrahydro-pyrimido-azepines are described. Representative compounds were shown to be subtype selective 5-HT2A antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Brock T. Shireman, Curt A. Dvorak, Dale A. Rudolph, Pascal Bonaventure, Diane Nepomuceno, Lisa Dvorak, Kirsten L. Miller, Timothy W. Lovenberg, Nicholas I. Carruthers,