Bioorganic and Medicinal Chemistry Letters p. 398 - 404 (2011)
Update date:2022-09-26
Topics:
Fader, Lee D.
Bethell, Richard
Bonneau, Pierre
B?s, Michael
Bousquet, Yves
Cordingley, Michael G.
Coulombe, René
Deroy, Patrick
Faucher, Anne-Marie
Gagnon, Alexandre
Goudreau, Nathalie
Grand-Ma?tre, Chantal
Guse, Ingrid
Hucke, Oliver
Kawai, Stephen H.
Lacoste, Jean-Eric
Landry, Serge
Lemke, Christopher T.
Malenfant, Eric
Mason, Stephen
Morin, Sébastien
O'Meara, Jeff
Simoneau, Bruno
Titolo, Steve
Yoakim, Christiane
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.
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