5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent Allosteric Site HIV-1 Integrase Inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY(2019)
摘要
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.
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关键词
inhibitors,integrase-allosteric-site
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