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Abstract

Synthesis and antiviral studies of novel N-sulphonamidomethyl piperazinyl fluoroquinolones

Author(s): P Selvam1, P Rathore1, S Karthikumar1, K Velkumar1, P Palanisamy1, S Vijayalakhsmi1, M Witvrouw2
1 Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankoil-626 190, India 2 Molecular Medicine, Katholieke Universiteit-Leuven and IRC KULAK, Kapucijnenvoer 33, B-3000 Leuven, Flanders, Belgium

Correspondence Address:
P Selvam Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankoil-626 190 India [email protected]


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 Î?M) most toxic compound in this series.

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