Login

Journal Image
Current Medicinal Chemistry
ISSN (Print): 0929-8673
ISSN (Online): 1875-533X
VOLUME: 7
ISSUE: 6
DOI: 10.2174/0929867003374886      Price:  $58









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

img
Author(s): Willard Lew, Xiaowu Chen and Choung U. Kim
Pages 663-672 (10)
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, 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
Affiliation:
Gilead Sciences Inc., 333 Lakeside Drive, Foster City, California 94404, USA