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Aromatic P 1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN®

CA Coburn, MB Young, RW Hungate…

文献索引:Coburn, Craig A.; Young, Mary Beth; Hungate, Randall W.; Isaacs, Richard C.A.; Vacca, Joseph P.; Huff, Joel R. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 16 p. 1937 - 1940

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被引用次数: 6

摘要

A series of analogs of CRIXIVAN® containing various aromatic P1 ligands were prepared and evaluated for inhibition of the HIV-1 protease enzyme. These new compounds were found to be effective inhibitors at nanomolar concentrations in the in vitro enzyme inhibition assay as well as the whole cell assay.