SYNTHESIS, ANTI-HIV AND CYTOTOXICITY STUDIES OF SOME NOVEL N-HETEROARYL METHYL PIPERAZINYL FLUOROQUINOLONE DERIVATIVES

Abstract

A series of novel N- substituted piperzinyl fluoroquinolones were synthesized and screened antiviral activity. 29 compounds were synthesized through modifying the N4-hydrogen of piperazine in fluoroquinolones with mannich reactions. The structures of the synthetic compounds were characterized by means of their IR, 1H-NMR data. The anti-HIV activities of the new compounds were screened antiviral activity against replication of HIV-1(III B) in MT-4 cells among the compounds tested two compounds, PD-NDIN and PD-CFA have shown more toxic in these series. Compounds PD-CDIN and PDNDIN exhibited 27 and 10 percent maximum protection against replication of HIV-1 in MT-4 cells at subtoxic concentration.