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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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

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

Volume 7, Issue 6, 2000

Page: [663 - 672] Pages: 10

DOI: 10.2174/0929867003374886

Price: $65


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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