Activity of isatine-sulfadimidine derivatives against 2009 pandemic H1N1 influenza virus in cell culture.
BACKGROUND
The development of antiviral drugs has provided crucial new means to mitigate or relieve the debilitating effects of many viral pathogens. New classes of inhibitors are essential to combat swine influenza viral infection.


METHODS
A series of isatine-sulfadimidine derivatives were screened for antiviral activity against swine influenza A/California/07/2009 (H1N1) virus in Madin-Darby canine kidney (MDCK) cell culture. Cytotoxicity of the synthesized compounds was also tested in uninfected MDCK cells.


RESULTS
All the compounds inhibit the influenza A (H1N1) in MDCK cells. The most active compounds, SPIII-5Br and SPIII-5H, inhibited virus-induced cytopathology by 50% at 27 and 30 microM, respectively, with 50% cytotoxicity occurring at a much higher dose (975-1,000 microM). The positive control compound ribavirin inhibits the replication of the virus at 18 microM and cytotoxic concentration was found to be >1,000 microM.


CONCLUSIONS
SPIII-5Br and SPIII-5H exhibited potency in the same range as ribavirin and are suitable candidate molecules for further investigation.
Selvam
Periyasamy
P
Devaki Amma Memorial College of Pharmacy, Chelembra, Kerala, India. periyasamy_selvam@yahoo.co.in
Chandramohan
Markandavel
M
Hurst
Brett L
BL
Smee
Donald F
DF
D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D004285:Dogs; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects* / Q000254:growth & development; D007251:Influenza, Human / Q000188:drug therapy* / Q000821:virology*; D013418:Sulfamethazine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013449:Sulfonamides / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D007211:Indoles; C516878:SPIII-5H; D013449:Sulfonamides; D013418:Sulfamethazine