alexa Abstract | Synthesis and antiviral studies of novel N-sulphonamidomethyl piperazinyl fluoroquinolones

Indian Journal of Pharmaceutical Sciences
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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 Î┬ůM) most toxic compound in this series.

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Author(s): P Selvam P Rathore S Karthikumar K Velkumar P Palanisamy S Vijayalakhsmi M Witvrouw

Keywords

Fluoroquinolone, Mannich reaction, antiHIV activity, Influenza, H5N1

 
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