Structure-based optimization and synthesis of antiviral drug Arbidol analogues with significantly improved affinity to influenza hemagglutinin

• Published in: Bioorganic & medicinal chemistry letters Vol. 27; no. 16; pp. 3744 - 3748
• Main Authors: Wright, Zoë V.F., Wu, Nicholas C., Kadam, Rameshwar U., Wilson, Ian A., Wolan, Dennis W.
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.08.2017; Elsevier
• Subjects: Antiviral Agents - chemical synthesis; Antiviral Agents - chemistry; Antiviral Agents - pharmacology; Arbidol; Bio-layer interferometry; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Crystallography, X-Ray; Dose-Response Relationship, Drug; Hemagglutinin; Hemagglutinins - metabolism; Humans; Indoles - chemical synthesis; Indoles - chemistry; Indoles - pharmacology; Influenza; Influenza, Human - drug therapy; Life Sciences & Biomedicine; Models, Molecular; Molecular Structure; Orthomyxoviridae - drug effects; Pharmacology & Pharmacy; Physical Sciences; Science & Technology; Structure-Activity Relationship; Structure-based drug design; Arbidol; Structure-based drug design; Bio-layer interferometry; Hemagglutinin; Influenza; IN-VITRO; FUSION; INHIBITION; A VIRUSES; RESISTANCE; OSELTAMIVIR

[Display omitted] Influenza is a highly contagious respiratory viral infection responsible for up to 50,000 deaths per annum in the US alone. The need for new therapeutics with novel modes of action is of paramount importance. We determined the X-ray structure of Arbidol with influenza hemagglutinin...