Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.

@article{Thaisrivongs1996StructurebasedDO,
  title={Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.},
  author={S Thaisrivongs and Donna L. Romero and Ruben A Tommasi and Meenakshi Janakiraman and Joseph W Strohbach and S R Turner and Charlie Biles and R R Morge and Paul D Johnson and Paul A. Aristoff and Paul K. Tomich and Jason Lynn and M.-S. Horng and Kok Ting Chong and Roger R. Hinshaw and W. J. Howe and Barry C. Finzel and Keith David Watenpaugh},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 23},
  pages={4630-42}
}
From a broad screening program, the 4-hydroxycoumarin phenprocoumon (I) was previously identified as a lead template with HIV protease inhibitory activity. The crystal structure of phenprocoumon/HIV protease complex initiated a structure-based design effort that initially identified the 4-hydroxy-2-pyrone U-96988 (II) as a first-generation clinical candidate for the potential treatment of HIV infection. Based upon the crystal structure of the 4-hydroxy-2-pyrone III/HIV protease complex, a… CONTINUE READING
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