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Keywords:

  • docking studies;
  • HIV-1;
  • noncompetitive inhibitors;
  • pyrimidinyl isoxazolidines;
  • reverse transcriptases
Thumbnail image of graphical abstract

Affairs of the HAART! The synthesis of HEPT-derived, truncated reverse isoxazolidinyl nucleosides (shown) is reported. These compounds represent the first examples of isoxazolidines bearing a pyrimidine scaffold at the C-3 position using a glycoside-type linkage. Biological evaluation showed that some of the derivatives act as non-nucleoside inhibitors of HIV-1 reverse transcriptase, with an efficacy comparable to that of Nevirapine but with reduced toxicity.