Current Medicinal Chemistry

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

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

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

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

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

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.

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Article Details

VOLUME: 7
ISSUE: 6
Page: [663 - 672]
Pages: 10
DOI: 10.2174/0929867003374886