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
Romano SilvestriPaolo La Colla

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.

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Citations

Aug 25, 2010·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Carrie DykesLisa M Demeter
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Apr 29, 2014·European Journal of Medicinal Chemistry·Valeria FamigliniRomano Silvestri
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