| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361943 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3′-processing.
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Authors
Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Metifiot, Steven J. Smith, B. Christie Vu, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. Burke Jr.,