| Autor: |
Silvestri, R., Artico, M., Martino, G. De, Regina, G. La, Loddo, R., Colla, M. La, Colla, P. La |
| Zdroj: |
Journal of Medicinal Chemistry; July 2004, Vol. 47 Issue: 15 p3892-3896, 5p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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