Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly.

2011 
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.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    13
    References
    81
    Citations
    NaN
    KQI
    []