Volume :
2
Issue :
4
Abstract :
A series of novel N-substituted piperazinyl fluoroquinolones were synthesized and screened for their antiviral activity and cytotoxicity. Twenty two derivatives of known fluoroquinolones (Ciprofloxacin, Norfloxacin, Sparfloxacin and Gatifloxacin) were synthesized by modifying the N4-hydrogen of piperazine in fluoroquinolone with Mannich reaction. The purity of the compounds was ascertained by consistency in the Rf value as well as melting point determination and were characterized by means of their spectral analysis (IR and 1H NMR). The anti-HIV activities of the derivatives were screened against replication of HIV-1(III B) and HIV-2(ROD) in MT-4 cells. The synthesized compounds were tested for antiviral activity against HeLa cells (VSV and RSV) HEL cells (HSV-1 and HSV-2) CRFK cells (Feline Corona and Feline Herpes Virus) and Vero cells (Para influenza-3, Reovirus-1, Sindbis virus, Coxsackie virus B4 and Punta Toro virus). Among the compounds, compound SF-2A4PT and GF-2A4PT exhibited anti-viral activity against Vesicular Stomatitis virus in HeLa cells at the concentration of 7µg/ml and 12µg/ml respectively, where as their cytotoxicity was found to be more than 100µg/ml. Compound SF-2A4PT also inhibit the replication of Respiratory Syncytial Virus (RSV) at the concentration of 45µg/ml and its cytotoxicity was found to be more than 100µg/ml. In–vitro cytotoxicity studies of the synthesized compounds were determined by using MTT assay in Human liver cancer cells (Hep G2 cells). All the tested compounds exhibited significant cytotoxicity. Hence these merits further investigation to screen its anti cancer activity using in-vitro and in-vivo models.