| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365704 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
A series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 6 is active against replication of HIV with a CIC95 of 0.31 μM and exhibits no shift in potency in the presence of 50% normal human serum. It displays a good pharmacokinetic profile when dosed in rats and no covalent binding with microsomal proteins in both in vitro and in vivo models.
Graphical abstractA series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells.Figure optionsDownload full-size imageDownload as PowerPoint slide
