| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375181 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
The synthesis and structure–activity relationships of the 4- and 6-substituents of 2,4-diaminopyrimidine-based growth hormone secretagogue receptor (GHS-R) antagonists are described. Diaminopyrimidines with 6-norbornenyl (4n) and 6-tetrahydrofuranyl (4p) substitutents were found to exhibit potent GHS-R antagonism and good selectivity (∼1000-fold) against dihydrofolate reductase.
Graphical abstractThe synthesis and structure–activity relationships of the 4- and 6-substituents of 2,4-diaminopyrimidine-based growth hormone secretagogue receptor (GHS-R) antagonists are described. Diaminopyrimidines with 6-norbornenyl (4n) and 6-tetrahydrofuranyl (4p) substitutents exhibited potent GHS-R antagonism and good selectivity (∼1000-fold) against dihydrofolate reductase.Figure optionsDownload full-size imageDownload as PowerPoint slide
