Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.

@article{Sun2005DesignSA,
  title={Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.},
  author={Chun-lai Sun and Ruifang Pang and H. Zhang and Ming Yang},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2005},
  volume={15 13},
  pages={
          3257-62
        }
}
Twenty-four 4-hydroxypyrone derivatives were synthesized with a facile synthetic method to develop novel HIV protease inhibitors. Most of them were shown to display good antiviral activities in SIV-infected CEM cells. The introduction of alpha-naphthylmethyl group to C-6 of 5,6-dihydropyran-2-ones led to an effective antiviral compound that showed an EC(50) value at 1.7 microM with a therapeutic index of 46. 
Isochromans and α-pyrones from Penicillium corylophilum.
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