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Discovery and Development of GS 4104 (oseltamivir) An Orally Active Influenza Neuraminidase Inhibitor

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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.

Keywords: GS 4104 oseltamivir; X ray crystal structures; active influenza neuraminidase inhibitors; carbocyclic influenza neuramindase inhibitors; carbocyclic inhibitors; influenza virus neuraminidase; inhibitor design; isosteres; sialic acid based; structure activity relationship

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867003374886

Publication date: June 1, 2000

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
ben/cmc/2000/00000007/00000006/art00005
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