| Literature DB >> 21087861 |
Lee D Fader1, Richard Bethell, Pierre Bonneau, Michael Bös, Yves Bousquet, Michael G Cordingley, René Coulombe, Patrick Deroy, Anne-Marie Faucher, Alexandre Gagnon, Nathalie Goudreau, Chantal Grand-Maître, Ingrid Guse, Oliver Hucke, Stephen H Kawai, Jean-Eric Lacoste, Serge Landry, Christopher T Lemke, Eric Malenfant, Stephen Mason, Sébastien Morin, Jeff O'Meara, Bruno Simoneau, Steve Titolo, Christiane Yoakim.
Abstract
The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione hit established structure-activity relationships. Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase. Optimization of the bicyclic benzodiazepine scaffold to include a 3-phenyl substituent led to lead compound 48, a pure capsid assembly inhibitor with improved antiviral activity.Entities:
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Year: 2010 PMID： 21087861 DOI： 10.1016/j.bmcl.2010.10.131
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823