Peramivir analogues bearing hydrophilic side chains exhibit higher activities against H275Y mutant than wild-type influenza virus.

@article{Chiu2017PeramivirAB,
  title={Peramivir analogues bearing hydrophilic side chains exhibit higher activities against H275Y mutant than wild-type influenza virus.},
  author={Din-Chi Chiu and Tzu-chen Lin and W. Huang and Ting-Jen Rachel Cheng and Keng-Chang Tsai and Jim-Min Fang},
  journal={Organic & biomolecular chemistry},
  year={2017},
  volume={15 46},
  pages={9910-9922}
}
Peramivir is an effective anti-influenza drug in the clinical treatment of influenza, but its efficacy toward the H275Y mutant is reduced. The previously reported cocrystal structures of inhibitors in the mutant neuraminidase (NA) suggest that the hydrophobic side chain should be at the origin of reduced binding affinity. In contrast, zanamivir having a hydrophilic glycerol side chain still possesses high affinity toward the H275Y NA. We thus designed five peramivir analogues (5-9) carrying… CONTINUE READING