Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.

@article{Wen2010AnalogsOZ,
  title={Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses.},
  author={W. Wen and Shi-Yun Wang and Keng-Chang Tsai and Y E Cheng and An-Suei Yang and Jim-Min Fang and C. -H. Wong},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 11},
  pages={4074-84}
}
Unlike the group-2 neuraminidase, the group-1 neuraminidase of influenza virus possesses a flexible loop (the 150-loop) and a cavity (the 150-cavity) adjacent to the active site, and renders a conformational change from the 'open' form to the 'closed' form on binding with substrate (sialo-glycoprotein) or inhibitor (e.g., zanamivir). Zanamivir derivative 8a having an extended (piperazinocarbonyl)propyl substituent at the internal N-position of the guanidino group is designed as a possible… CONTINUE READING