From neuraminidase inhibitors to conjugates: a step towards better anti-influenza drugs?

Abstract

For the treatment of seasonal flu and possible pandemic infections the development of new anti-influenza drugs that have good bioavailability against a broad spectrum of influenza viruses including the resistant strains is needed. In this review, we summarize previous methods for the structural modification of zanamivir, a potent neuraminidase inhibitor that has rare drug resistance, in order to develop effective anti-influenza drugs. We also report recent research into the design of multivalent zanamivir drugs and bifunctional zanamivir conjugates, some of which have shown better efficacy in animal experiments. As a step towards developing improved antivirals, conjugating anti-influenza drugs with anti-inflammatory agents can improve oral bioavailability and also exert synergistic effect in influenza therapy.

• Authors: Chung-Kai Cheng, Chen-Hsuan Tsai, Jiun-Jie Shie, Jim-Min Fang
• Journal: Future medicinal chemistry (Future Med Chem) Vol. 6 Issue 7 Pg. 757-74 (May 2014) ISSN: 1756-8927 [Electronic] England
• PMID: 24941871 (Publication Type: Journal Article, Review)

Chemical References

• Antiviral Agents
• Enzyme Inhibitors
• Neuraminidase
• Zanamivir

Topics

• Animals
• Antiviral Agents (chemistry, pharmacology)
• Drug Design
• Enzyme Inhibitors (chemistry, pharmacology)
• Humans
• Influenza, Human (drug therapy, enzymology, virology)
• Molecular Targeted Therapy
• Neuraminidase (antagonists & inhibitors, chemistry, metabolism)
• Orthomyxoviridae (drug effects, enzymology, physiology)
• Orthomyxoviridae Infections (drug therapy, enzymology, virology)
• Zanamivir (analogs & derivatives, pharmacology)