title: Identification of small molecules acting against H1N1 influenza A virus.
abstract: Influenza virus represents a serious threat to public health. The lack of effective drugs against flu prompted researchers to identify more promising viral target. In this respect hemagglutinin (HA) can represent an interesting option because of its pivotal role in the infection process. With this aim we collected a small library of commercially available compounds starting from a large database and performing a diversity-based selection to reduce the number of screened compounds avoiding structural redundancy of the library. Selected compounds were tested for their hemagglutination-inhibiting (HI) ability against two different A/H1N1 viral strains (one of which is oseltamivir sensitive), and 17 of them showed the ability to interact with HA. Five drug-like molecules, in particular, were able to impair hemagglutination of both A/H1N1 viral strains under study and to inhibit cytopathic effect and hemolysis at sub-micromolar level.
authors.affiliation: Department of Pharmacy, University "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Mariangela
authors.initials: M
authors.lastname: Agamennone
authors.affiliation: Department of Technology and Health, National Institute of Health, Viale Regina Elena 299, 00161 Rome, Italy.
authors.forename: Agostina
authors.initials: A
authors.lastname: Pietrantoni
authors.affiliation: Department of Technology and Health, National Institute of Health, Viale Regina Elena 299, 00161 Rome, Italy. Electronic address: fabiana.superti@iss.it.
authors.forename: Fabiana
authors.initials: F
authors.lastname: Superti
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D003588:Cytopathogenic Effect, Viral; D004285:Dogs; D004353:Drug Evaluation, Preclinical / Q000379:methods; D019267:Hemagglutinin Glycoproteins, Influenza Virus / Q000378:metabolism*; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects*; D061985:Madin Darby Canine Kidney Cells
chemical_list: D000998:Antiviral Agents; C543345:H1N1 virus hemagglutinin; D019267:Hemagglutinin Glycoproteins, Influenza Virus
keywords: Diverse library; Fusion peptide; Hemagglutinin; Hemolysis; Influenza