Oximinoarylsulfonamides as potent HIV protease inhibitors

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• 作者：Yeung ; Clinton M. ; Klein ; Larry L. ; Flentge ; Charles A. ; Randolph ; John T. ; Zhao ; Chen ; Sun ; MingHua ; et. al.
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：May 2, 2005
• 年：2005
• 卷：15
• 期：9
• 页码：2275-2278
• 全文大小：185 K

文摘

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 structureaaaactivity relationships (SAR) based upon the in vitro IC₅₀ of this series of compounds are reported.