tailieunhanh - Synthesis and characterization of N-Mannich based prodrugs of ciprofloxacin and norfloxacin: In vitro anthelmintic and cytotoxic evaluation

Prodrugs, the inert derivatives of existing drugs have successfully contributed to the modification of their physicochemical properties. The improved antimicrobial potential due to enhanced lipophilicity of some of the synthesized prodrugs of antibacterial agents by various schemes has already been reported. In the current study, synthesis, characterization, and biological evaluation of some more lipid based prodrugs/- compounds of ciprofloxacin and norfloxacin has been carried out. The synthesized prodrugs/compounds have been screened for anthelmintic activity using Indian earthworms and cytotoxic activity against human lung cancer cell lines A-549 employing sulforhodamine B (SRB) assay method. The prodrugs FQF1, 6b, 6c, and 6k were found to possess promising anthelmintic activity due to improved partition coefficient. Growth of selected cells lines was found to decrease with increase in concentration of prodrugs as compared to parent drug. Prodrug, 6k having GI50 value , has been proved to be the most active among all the synthesized prodrugs. Results of present investigation reveal that some of the synthesized prodrugs/compounds were found to possess promising biological activity. | Synthesis and characterization of N-Mannich based prodrugs of ciprofloxacin and norfloxacin: In vitro anthelmintic and cytotoxic evaluation