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

Silvestri, R; Artico, M; De Martino, G; La Regina, G; Loddo, Roberta; La Colla, M; Mura, M; La Colla, P.

doi:10.1021/jm031147e

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 a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations / SILVESTRI R; ARTICO M; DE MARTINO G; LA REGINA G; LODDO R; LA COLLA M; MURA M; LA COLLA P. - 47:15(2004), pp. 3892-3896.

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Titolo:	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
Autori:	SILVESTRI R ARTICO M DE MARTINO G LA REGINA G LODDO, ROBERTA LA COLLA M MURA M LA COLLA P. mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2004
Rivista:	JOURNAL OF MEDICINAL CHEMISTRY
Citazione:	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 / SILVESTRI R; ARTICO M; DE MARTINO G; LA REGINA G; LODDO R; LA COLLA M; MURA M; LA COLLA P. - 47:15(2004), pp. 3892-3896.
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.
Handle:	http://hdl.handle.net/11584/12875
Tipologia:	1.1 Articolo in rivista

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