| Literature DB >> 18215014 |
Xiongyu Wu1, Per Ohrngren, Jenny K Ekegren, Johan Unge, Torsten Unge, Hans Wallberg, Bertil Samuelsson, Anders Hallberg, Mats Larhed.
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.Entities:
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Year: 2008 PMID： 18215014 DOI： 10.1021/jm070680h
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446