Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.

@article{Hsu2018AcylguanidineDO,
  title={Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses.},
  author={Peng-Hao Hsu and Din-Chi Chiu and Kuan-Lin Wu and Pei-Shan Lee and J T Jan and Yih-Shyun E. Cheng and Keng-Chang Tsai and Ting-Jen Rachel Cheng and Jim-Min Fang},
  journal={European journal of medicinal chemistry},
  year={2018},
  volume={154},
  pages={
          314-323
        }
}
Zanamivir (ZA) and guanidino-oseltamivir carboxylic acid (GOC) are very potent inhibitors against influenza neuraminidase (NA). The guanidinium moiety plays an important role in NA binding; however, its polar cationic nature also hinders the use of ZA and GOC from oral administration. In this study, we investigated the use of ZA and GOC acylguanidine derivatives as possible orally available prodrugs. The acylguanidine derivatives were prepared by coupling with either n-octanoic acid or (S… 
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