Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


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

Author(s): Willard Lew, Xiaowu Chen, Choung U. Kim.


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, active influenza neuraminidase inhibitors, X ray crystal structures, influenza virus neuraminidase, sialic acid based, inhibitor design, structure activity relationship, carbocyclic inhibitors, isosteres, carbocyclic influenza neuramindase inhibitors

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Article Details

Year: 2000
Page: [663 - 672]
Pages: 10
DOI: 10.2174/0929867003374886
Price: $58