Bioorganic & Medicinal Chemistry Letters 2004-02-23

Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.

John F Miller, Eric S Furfine, Mary H Hanlon, Richard J Hazen, John A Ray, Laurence Robinson, Vicente Samano, Andrew Spaltenstein

文献索引：Bioorg. Med. Chem. Lett. 14 , 959-963, (2004)

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摘要

A novel series of P1' chain-extended arylsufonamides was synthesized and evaluated for wild-type HIV protease inhibitory activity and in vitro antiviral activity against wild type virus and two protease inhibitor-resistant mutant viruses. All of the compounds showed dramatic increases in enzyme activity as compared to the currently marketed HIV protease inhibitors amprenavir, indinavir, and nelfinavir. In addition, significant improvements in antiviral potencies against wild type and the two mutant viruses were also realized.