Article
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
Journal of medicinal chemistry - 10 Aug 2017
Famiglini Valeria, La Regina Giuseppe, Coluccia Antonio, Masci Domiziana, Brancale Andrea, Badia Roger, Riveira-Muñoz Eva, Esté José A, Crespan Emmanuele, Brambilla Alessandro, Maga Giovanni, Catalano Myriam, Limatola Cristina, Formica Francesca Romana, Cirilli Roberto, Novellino Ettore, Silvestri Romano
Abstract excerpt
We designed and synthesized a series of chiral indolyarylsulfones (IASs) as new HIV-1 NNRTIs. The new IASs 8-37 showed potent inhibition of the HIV-1 WT NL4-3 strain and of the mutant K103N, Y181C, Y188L, and K103N-Y181C HIV-1 strains. Six racemic mixtures, 8, 23-25, 31, and 33, were separated at semipreparative level into their pure enantiomers. The (R)-8 enantiomer bearing the chiral (α-methylbenzyl) was...
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