Curr Med Chem. 2000 Jun;7(6):663-72.

Discovery and development of GS 4104 (oseltamivir): an orally active influenza neuraminidase inhibitor.

Source

Gilead Sciences Inc., 333 Lakeside Drive, Foster City, California, 94404, USA.

Abstract

Rational drug design utilizing available X-ray crystal structures of sialic acid analogues bound to the active site of influenza virus neuraminidase has led to the discovery of a series of potent carbocyclic influenza neuraminidase inhibitors. From this series, GS 4104 (oseltamivir, TAMIFLU ) has emerged as a promising antiviral for the treatment and prophylaxis of human influenza infection. This article will summarize the design, discovery, and development of oseltamivir as an oral therapeutic to treat influenza infection.

PMID:: 10702632; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Supplemental Content

Icon for Bentham Science Publishers Ltd.

Save items

Related citations in PubMed

Review Neuraminidase inhibitors as anti-influenza virus agents. [Antivir Chem Chemother. 1999]
Review Neuraminidase inhibitors as anti-influenza virus agents.
Kim CU, Chen X, Mendel DB. Antivir Chem Chemother. 1999 Jul; 10(4):141-54.
Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors. [J Med Chem. 1998]
Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors.
Kim CU, Lew W, Williams MA, Wu H, Zhang L, Chen X, Escarpe PA, Mendel DB, Laver WG, Stevens RC. J Med Chem. 1998 Jul 2; 41(14):2451-60.
Influence of treatment schedule and viral challenge dose on the in vivo influenza virus-inhibitory effects of the orally administered neuraminidase inhibitor GS 4104. [Antivir Chem Chemother. 1999]
Influence of treatment schedule and viral challenge dose on the in vivo influenza virus-inhibitory effects of the orally administered neuraminidase inhibitor GS 4104.
Sidwell RW, Bailey KW, Bemis PA, Wong MH, Eisenberg EJ, Huffman JH. Antivir Chem Chemother. 1999 Jul; 10(4):187-93.
Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. [Antimicrob Agents Chemother. 2...]
Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir.
Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, Chand P, Kotian PL, Dehghani A, El-Kattan Y, Lin T, et al. Antimicrob Agents Chemother. 2001 Apr; 45(4):1162-7.
Review Different synthetic strategies of oseltamivir phosphate: a potent influenza neuraminidase inhibitor. [Curr Med Chem. 2008]
Review Different synthetic strategies of oseltamivir phosphate: a potent influenza neuraminidase inhibitor.
Gong J, Xu W. Curr Med Chem. 2008; 15(30):3145-59.

See reviews... See all...

Cited by 11 PubMed Central articles

Tamiflu-resistant but HA-mediated cell-to-cell transmission through apical membranes of cell-associated influenza viruses. [PLoS One. 2011]
Tamiflu-resistant but HA-mediated cell-to-cell transmission through apical membranes of cell-associated influenza viruses.
Mori K, Haruyama T, Nagata K. PLoS One. 2011; 6(11):e28178. Epub 2011 Nov 30.
Using Selectively Applied Accelerated Molecular Dynamics to Enhance Free Energy Calculations. [J Chem Theory Comput. 2010]
Using Selectively Applied Accelerated Molecular Dynamics to Enhance Free Energy Calculations.
Wereszczynski J, McCammon JA. J Chem Theory Comput. 2010 Nov 9; 6(11):3285-3292. Epub 2010 Oct 13.
Antiviral effects of a transgenic RNA-dependent RNA polymerase. [J Virol. 2011]
Antiviral effects of a transgenic RNA-dependent RNA polymerase.
Kerkvliet J, Papke L, Rodriguez M. J Virol. 2011 Jan; 85(1):621-5. Epub 2010 Oct 20.

See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Discovery and development of GS 4104 (oseltamivir): an orally active influenza n...
Discovery and development of GS 4104 (oseltamivir): an orally active influenza neuraminidase inhibitor.
Curr Med Chem. 2000 Jun ;7(6):663-72.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to:

Discovery and development of GS 4104 (oseltamivir): an orally active influenza neuraminidase inhibitor.

Source

Abstract

Publication Types, MeSH Terms, Substances

Publication Types

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Supplemental Content

Save items

Related citations in PubMed

Cited by 11 PubMed Central articles

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information