1. Discovery and Development of GS 4104 (oseltamivir) An Orally Active Influenza Neuraminidase Inhibitor
- Author
-
Choung U. Kim, Willard Lew, and Xiaowu Chen
- Subjects
Oseltamivir ,Orthomyxoviridae ,Administration, Oral ,Neuraminidase ,Drug design ,Antiviral Agents ,Biochemistry ,Virus ,Structure-Activity Relationship ,chemistry.chemical_compound ,Drug Discovery ,Animals ,Humans ,Amines ,Enzyme Inhibitors ,Pharmacology ,biology ,Organic Chemistry ,virus diseases ,Prodrug ,biology.organism_classification ,Virology ,Sialic acid ,chemistry ,Enzyme inhibitor ,Drug Design ,Immunology ,biology.protein ,Molecular Medicine - 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.
- Published
- 2000
- Full Text
- View/download PDF