Article
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
Journal of medicinal chemistry - 26 Feb 2009
Butini Stefania, Brindisi Margherita, Cosconati Sandro, Marinelli Luciana, Borrelli Giuseppe, Coccone Salvatore Sanna, Ramunno Anna, Campiani Giuseppe, Novellino Ettore, Zanoli Samantha, Samuele Alberta, Giorgi Gianluca, Bergamini Alberto, Di Mattia Michela, Lalli Silvana, Galletti Bruno, Gemma Sandra, Maga Giovanni
Abstract excerpt
Starting from the prototypic compound 4, we describe new, potent, and broad-spectrum pyrrolobenzo(pyrido)oxazepinones antivirals. A biochemical and enzymological investigation was performed for defining their mechanism of inhibition at either recombinant HIV-1 RT wild type and non-nucleoside reverse transcriptase inhibitors (NNRTIs)-resistant mutants. For the novel compounds (S)-(+)-5 and (S)-(-)-7, a clear-cut...
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