Anti-picornavirus activity of synthetic flavon-3-yl esters.
The in vitro antiviral activity against picornaviruses (rhinovirus serotype 1B and 14, and poliovirus type 2) of new synthetic 3-hydroxyflavones, 3-acetoxyflavones, and substituted cinnamic and benzoic acid flavon-3-yl esters was evaluated. The maximum non-toxic concentration of compounds was determined in a human cell line (HeLa) suitable for the replication of the three viruses. Their antiviral potency was measured by a plaque reduction assay. Generally, rhinoviruses exhibited a higher sensitivity to the new flavonoids than poliovirus. Flavones, with sterically small substituents in position 3, showed good activity against both rhinoviruses tested. However, the introduction of bulky substituents in the same position resulted in analogues with a higher toxicity and often with a lower efficacy.
Conti
C
C
Institute of Microbiology, School of Medicine, Rome, Italy. desideri@axrma.uniroma1.it
Mastromarino
P
P
Sgro
R
R
Desideri
N
N
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology*; D002934:Cinnamates / Q000138:chemical synthesis / Q000494:pharmacology*; D003373:Coumaric Acids / Q000138:chemical synthesis / Q000494:pharmacology; D004951:Esterification; D005419:Flavonoids / Q000138:chemical synthesis / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D062385:Hydroxybenzoates / Q000138:chemical synthesis; D015394:Molecular Structure; D017955:Poliovirus / Q000187:drug effects* / Q000502:physiology; D012229:Rhinovirus / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship; D010948:Viral Plaque Assay; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D001565:Benzoates; D002934:Cinnamates; D003373:Coumaric Acids; D005419:Flavonoids; D062385:Hydroxybenzoates