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, K103N-Y181C, and triple mutant (K103R, V179D, P225H) highly resistant to efavirenz] superior to that of the parent indole derivative 1.
Simple, Short Peptide Derivatives of L-737,126 Active In Vitro Against HIV-1 WT and Variants Carrying NNRTI Resistance Mutations / Silvestri, Romano; Artico, Marino; DE MARTINO, G.; LA REGINA, Giuseppe; Loddo, R.; LA COLLA, M.; Mura, M.; LA COLLA, P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 47:(2004), pp. 3892-3896. [10.1021/jm031147e]
Simple, Short Peptide Derivatives of L-737,126 Active In Vitro Against HIV-1 WT and Variants Carrying NNRTI Resistance Mutations.
SILVESTRI, Romano;ARTICO, Marino;LA REGINA, GIUSEPPE;
2004
Abstract
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, K103N-Y181C, and triple mutant (K103R, V179D, P225H) highly resistant to efavirenz] superior to that of the parent indole derivative 1.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
