5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors
Copyright policy )5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for activity against HIV-1 infection in cell culture. Small molecules that bind within the LEDGF/p75-binding site promote aberrant multimerization of the integrase enzyme and are of significant interest as HIV-1-replication inhibitors. Structure-activity-relationship studies and rat pharmacokinetic studies of lead compounds are presented.
- GlaxoSmithKline (United States) United States
- Cellzome, GSK, Middlesex, UK.
HIV-1, Humans, HIV Infections, HIV Integrase Inhibitors, Naphthyridines, Crystallography, X-Ray, Virus Replication, Allosteric Site
HIV-1, Humans, HIV Infections, HIV Integrase Inhibitors, Naphthyridines, Crystallography, X-Ray, Virus Replication, Allosteric Site
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