Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372689 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell. Integrase inhibitor N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide selectively inhibits the strand transfer process of integration. 4-Substituted pyrrolidinones possessing various groups on the pyrrolidinone nitrogen were introduced at the 5-position of the naphthyridine scaffold. These analogs exhibit excellent activity against viral replication in a cell-based assay. The preparation of these compounds was enabled by a three-step, two-pot reaction sequence from a common butenolide intermediate.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey Y. Melamed, Melissa S. Egbertson, Sandor Varga, Joseph P. Vacca, Greg Moyer, Lori Gabryelski, Peter J. Felock, Kara A. Stillmock, Marc V. Witmer, William Schleif, Daria J. Hazuda, Yvonne Leonard, Lixia Jin, Joan D. Ellis, Steven D. Young,