Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364961 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of Isentress™, represents a validated target for anti-retroviral therapy. Incorporation of the dihydroxycarbonyl pharmacophore into a pyrrolinone scaffold led to the discovery of 5-pyrrolinone-3-carboxamides as a structurally diverse class of HIV-1 integrase inhibitors.
Graphical abstractA series of novel 4-hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors was identified. SAR around the pyrrolinone core resulted in the discovery of compounds with inhibitory activity in the low nanomolar range.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Paola Pace, Stéphane A.H. Spieser, Vincenzo Summa,