Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: The discovery of GW0385

John F. Miller,C. Webster Andrews,Michael Brieger,Eric S. Furfine,Michael R. Hale,Mary H. Hanlon,Richard J. Hazen,Istvan Kaldor,Ed W. McLean,David Reynolds,Douglas M. Sammond,Andrew Spaltenstein,Roger Tung,Elizabeth M. Turner,Robert X. Xu,Ronald G. Sherrill

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.

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关键词

Antiviral,Antiretroviral,Arylsulfonamide,Brecanavir,Drug resistance,GW0385,HIV protease

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