Article
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
Journal of medicinal chemistry - 15 Jul 2004
Silvestri Romano, Artico Marino, De Martino Gabriella, La Regina Giuseppe, Loddo Roberta, La Colla Massimiliano, Mura Massimo, La Colla Paolo
Abstract excerpt
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) active against NNRTI-resistant mutants were obtained by introducing two methyl groups at positions 3 and 5 of the benzenesulfonyl moiety of L-737,126 (1) and coupling one to three glycinamide/alaninamide units to its carboxyamide function. In cell-based assays, the new derivatives showed activities against HIV-1 wild type and NNRTI-resistant mutants [Y181C,...
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