1yt9
HIV Protease with oximinoarylsulfonamide bound
OverviewOverview
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.
About this StructureAbout this Structure
1YT9 is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.
ReferenceReference
Oximinoarylsulfonamides as potent HIV protease inhibitors., Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8. PMID:15837308 Page seeded by OCA on Sat May 3 16:45:37 2008