| Literature DB >> 30609350 |
Kevin M Peese, Christopher W Allard, Timothy Connolly, Barry L Johnson, Chen Li, Manoj Patel, Margaret E Sorensen, Michael A Walker, Nicholas A Meanwell, Brian McAuliffe, Beatrice Minassian, Mark Krystal, Dawn D Parker, Hal A Lewis, Kevin Kish, Ping Zhang, Robert T Nolte1, Jean Simmermacher, Susan Jenkins, Christopher Cianci, B Narasimhulu Naidu.
Abstract
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.Entities:
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Year: 2019 PMID： 30609350 DOI： 10.1021/acs.jmedchem.8b01473
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446