Document Report Card

ID: ALA1143221

Journal: J Med Chem

Title: Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.

Authors: Wu X, Ohrngren P, Ekegren JK, Unge J, Unge T, Wallberg H, Samuelsson B, Hallberg A, Larhed M.

Abstract: A new generation of HIV-1 protease inhibitors encompassing a tertiary-alcohol-based transition-state mimic has been developed. By elongation of the core structure of recently reported inhibitors with two carbon atoms and by varying the P1' group of the compounds, efficient inhibitors were obtained with Ki down to 2.3 nM and EC50 down to 0.17 microM. Two inhibitor-enzyme X-ray structures are reported.

CiteXplore: 18215014

DOI: 10.1021/jm070680h