title: Synthesis and Antiviral Studies of Novel N-Sulphonamidomethyl piperazinyl Fluoroquinolones.
abstract: A series of novel N-Sulphonamidomethyl piperzinyl fluoroquinolones were synthesized and screened antiviral activity. Eight compounds were synthesized through modifying the N(4)-hydrogen of piperazine in fluoroquinolones with formaldehyde and sulphanomides by Mannich reactions. The structures of the synthesized compounds were characterized by means of their IR and (1)H-NMR spectral data. Synthesized compounds were screened for antiviral activity against influenza A (H1N1, H3N2, H5N1) and influenza B viruses in MDCK cell culture. The antiHIV activities of the new compounds were screened for antiviral activity against replication of HIV-1(III(B)) in MT-4 cells. Cytotoxicity of the synthesized compounds was also tested in mock-infected MDCK and MT-4 cells. Compound CF-SD and CF-SDM inhibits the influenza A (H1N1) and compound GF-SDM inhibit the replication of influenza A (H5N1) and B in MDCK cells. All compounds displayed cytostatic propertity in MT-4 cells. Among the compounds tested, GF-SDM (CC(50)=39.44 muM) most toxic compound in this series.
authors.affiliation: Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankoil-626 190, India.
authors.forename: P
authors.initials: P
authors.lastname: Selvam
authors.forename: P
authors.initials: P
authors.lastname: Rathore
authors.forename: S
authors.initials: S
authors.lastname: Karthikumar
authors.forename: K
authors.initials: K
authors.lastname: Velkumar
authors.forename: P
authors.initials: P
authors.lastname: Palanisamy
authors.forename: S
authors.initials: S
authors.lastname: Vijayalakhsmi
authors.forename: M
authors.initials: M
authors.lastname: Witvrouw