title: Short communication inhibitory activity of 4-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)amino]-N-(4,6-dimethylpyrimidin-2-yl) benzenesulphonamide and its derivatives against orthopoxvirus replication in vitro.
abstract: 4-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)amino]-N-(4,6-dimethylpyrimidin-2-yl) benzenesulphonamide and its derivatives were tested in vitro for antiviral activity against vaccinia and cowpox virus replication in human foreskin fibroblast (HFF) cells, and their activity was compared with cidofovir (CDV). Among the tested compounds, 4-[(5-methyl-1,2-dihydro-2-oxo-3-H-indol-3-ylidene)amino]-N-(4,6-dimethylpyrimidin-2-yl)benzene-sulphonamide was the most active against vaccinia virus, with a 50% effective concentration (EC50) value of 18 microM and 4-[(N-acetyl-1,2-dihydro-2-oxo-3-H-indol-3-ylidene)amino]-N-(4,6-dimethylpyrimidin-2-yl) benzenesulphonamide was the most active against cowpox virus (EC50=33 microM). Cidofovir was found to have an EC50 of 20 microM and 32 microM against vaccinia and cowpox virus, respectively. Most of the tested compounds were non-cytotoxic (>300 microM) in HFF cells as determined by a neutral red uptake assay. The substitution of a halogen atom at the 5-position of isatin abolished the antiviral activity.
authors.affiliation: Arulmigu Kalasalingam College of Pharmacy, Anandnagar, Krishnankoil, Tamilnadu, India. periyasamyselvam2001@yahoo.co.in
authors.forename: Periyasamy
authors.initials: P
authors.lastname: Selvam
authors.forename: Narayanan
authors.initials: N
authors.lastname: Murugesh
authors.forename: Markandavel
authors.initials: M
authors.lastname: Chandramohan
authors.forename: Kathy A
authors.initials: KA
authors.lastname: Keith
authors.forename: Earl R
authors.initials: ER
authors.lastname: Kern
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D006801:Humans; D007211:Indoles / Q000494:pharmacology*; D018155:Orthopoxvirus / Q000187:drug effects* / Q000502:physiology; D013449:Sulfonamides / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects*; D000096926:Benzenesulfonamides
chemical_list: D000998:Antiviral Agents; D007211:Indoles; D013449:Sulfonamides; C515014:4-((5-methyl-1,2-dihydro-2-oxo-3H-indol-3-ylidene)amino)-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide; D000096926:Benzenesulfonamides; C515015:4-((N-acetyl-1,2-dihydro-2-oxo-3H-indol-3-ylidene)amino)-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide