|
|||||
|
|
Efficient Synthesis of Highly Active Phospha‐Isosteres of the Influenza Neuraminidase Inhibitor Oseltamivir |
|
| Authors: | Benoit Carbain Patrick J. Collins Dr. Lori Callum Stephen R. Martin Dr. Alan J. Hay Dr. John McCauley Dr. Hansjörg Streicher Dr. |
| Affiliation: | 1. Department of Chemistry and Biochemistry, University of Sussex, Brighton, BN1?9QG (UK), Fax: (+44)?1273‐876687, Homepage: http://www.sussex.ac.uk/chemistry;2. Division of Virology, National Institute of Medical Research, Mill Hill, London NW7?1AA (UK) |
| Abstract: | With a Hunsdiecker–Barton iododecarboxylation strategy, we converted the carboxylate group of the oseltamivir precursor into exemplary phosphonate monoesters. In all cases, Ki values towards influenza virus sialidase remained in the sub‐nanomolar range. We have thus made valuable structural space available for the design of novel oseltamivir‐based tools for influenza virus research.  |
| Keywords: | antiviral agents influenza inhibitors oseltamivir sialic acid sialylmimetics |