title: (E)-2-styrylchromones as potential anti-norovirus agents.
abstract: Human noroviruses (NoV) are now recognized as the most frequent cause of outbreaks and sporadic cases of acute gastroenteritis. Despite the significant economic impact and considerable morbidity of norovirus disease, no drug or vaccine is currently available to treat or prevent this disease, therefore the discovery of anti-norovirus drugs is urgent. In the present work, a total of 12 structure related chromone and (E)-2-styrylchromones were evaluated for their potential anti-norovirus activity using the murine norovirus (MNV) as a surrogate model for human NoV. From the 12 compounds studied, six (E)-2-styrylchromones were found to have with interesting anti-norovirus activity. The best compounds of the series were (E)-5-hydroxy-2-styrylchromone and (E)-4'-methoxy-2-styrylchromone with an IC(50) approximately 7muM. A first insight into the mechanism of action of these compounds was possible. An interesting relationship between the anti-norovirus activity and the chemical structure was observed. The present study points out that the (E)-2-styrylchromones skeleton is an important one which deserves to be developed and further explored as new antiviral drugs against NoV.
authors.affiliation: Serviço de Microbiologia, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha, Porto, Portugal.
authors.forename: Joana
authors.initials: J
authors.lastname: Rocha-Pereira
authors.forename: Ricardo
authors.initials: R
authors.lastname: Cunha
authors.forename: Diana C G A
authors.initials: DC
authors.lastname: Pinto
authors.forename: Artur M S
authors.initials: AM
authors.lastname: Silva
authors.forename: Maria São José
authors.initials: MS
authors.lastname: Nascimento
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D017250:Caliciviridae Infections / Q000188:drug therapy; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D004195:Disease Models, Animal; D005759:Gastroenteritis / Q000188:drug therapy; D006801:Humans; D051379:Mice; D029322:Norovirus / Q000187:drug effects*; D013237:Stereoisomerism; D013343:Styrenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use
chemical_list: C528112:4'-methoxy-2-styrylchromone; C552759:5-hydroxy-2-styrylchromone; D000998:Antiviral Agents; D002867:Chromones; D013343:Styrenes