Description and references

Orally active inhibitor of influenza virus neuraminidase; converted in vivo to the active acid metabolite, GS-4071. Prepn: N. W. Bischofberger et al., US 5763483 (1998 to Gilead Sci.). Improved prepn: Y.-Y. Yeung et al., J. Am. Chem. Soc. 128, 6310 (2006). Degradation kinetics: R. Oliyai et al., Pharm. Res. 15, 1300 (1998). Bioavailability and pharmacokinetics: W. Li et al., Antimicrob. Agents Chemother. 42, 647 (1998). Review of structure-activity studies and clinical development: C. U. Kim, Med. Chem. Res. 8, 392-399 (1998). Clinical trial in prevention of influenza: F. G. Hayden et al., N. Engl. J. Med. 341, 1336 (1999); in treatment of acute influenza: J. J. Treanor et al., J. Am. Med. Assoc. 283, 1016 (2000). Review of potential use in influenza pandemic: P. Ward et al., J. Antimicrob. Chemother. 55, Suppl. S1, i5-i21 (2005).

Properties

Derivative