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
- 22 June 2004
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (15) , 3892-3896
- https://doi.org/10.1021/jm031147e
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.Keywords
This publication has 6 references indexed in Scilit:
- HIV and AIDS: looking aheadNature Medicine, 2003
- Highlights in the development of new antiviral agents.Mini-Reviews in Medicinal Chemistry, 2002
- Non-Nucleoside Reverse Transcriptase Inhibitors: The NNRTI BoomAntiviral Chemistry and Chemotherapy, 1999
- Non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of human immunodeficiency virus type 1 (HIV-1) infections: Strategies to overcome drug resistance developmentMedicinal Research Reviews, 1996
- 2-Sulfonyl-4-chloroanilino Moiety: A Potent Pharmacophore for the Anti-Human Immunodeficiency Virus Type 1 Activity of Pyrrolyl Aryl SulfonesJournal of Medicinal Chemistry, 1996
- Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compoundsJournal of Virological Methods, 1988