Oximinoarylsulfonamides as potent HIV protease inhibitors.
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Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ
Oximinoarylsulfonamides as potent HIV protease inhibitors.
Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8.
- PubMed ID
- 15837308 [ View in PubMed]
- Abstract
The need for a potent HIV protease inhibitor (PI) to combat emerging PI-resistant viruses is anticipated. Analogs formulated from the combination of structural fragments of Ritonavir, Lopinavir, and Amprenavir were synthesized. Analogs containing the oxime pharmacophore were found to have improved activities against both wild type and resistant (A17) viruses. The synthesis and structure-activity relationships (SAR) based upon the in vitro IC50 of this series of compounds are reported.