| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366083 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. Previous reports have demonstrated that the diketoacid-based chemotype is a useful starting point for the design of inhibitors of this enzyme. In this study, one of the ketone groups is replaced by a benzylamide resulting in a new potent chemotype. A preliminary SAR study is carried out to investigate the substitution requirements on the phenyl ring and methylene group of the benzylamide.
Graphical abstractSAR study of benzyl amide-ketoacid based chemotype yielded highly active inhibitors of the HIV-integrase.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael A. Walker, Timothy Johnson, B. Narasimhulu Naidu, Jacques Banville, Roger Remillard, Serge Plamondon, Alain Martel, Chen Li, Albert Torri, Himadri Samanta, Zeyu Lin, Ira Dicker, Mark Krystal, Nicholas A. Meanwell,