title: A rigid bicyclic platform for the generation of conformationally locked neuraminidase inhibitors.
abstract: Rapid mutation of the influenza virus through genetic mixing raises the prospect of new strains that are both highly transmissible and highly lethal, and which have the ability to evade both immunization strategies (through mutation of hemagglutinin) and current therapies (through mutation of neuraminidase). Inspired by a need for next-generation therapeutics, a synthetic strategy for a new class of rigid, bicyclic inhibitors of influenza neuraminidase is reported.
authors.affiliation: Department of Chemistry, University of Victoria, Victoria, BC, Canada, V8W 3V6.
authors.forename: Michael G
authors.initials: MG
authors.lastname: Brant
authors.forename: Jeremy E
authors.initials: JE
authors.lastname: Wulff
mesh_terms: D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry; D019267:Hemagglutinin Glycoproteins, Influenza Virus / Q000235:genetics; D006388:Hemagglutinins / Q000235:genetics; D006801:Humans; D053118:Influenza A Virus, H1N1 Subtype / Q000235:genetics; D053124:Influenza A Virus, H5N1 Subtype / Q000235:genetics; D007251:Influenza, Human / Q000235:genetics; D020128:Inhibitory Concentration 50; D009154:Mutation; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000276:immunology
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D019267:Hemagglutinin Glycoproteins, Influenza Virus; D006388:Hemagglutinins; D009439:Neuraminidase