Polymeric prodrugs containing neridronate and ferrocene: Synthesis, characterization, and antimalarial activity

Polyamidoamine prodrugs containing ferrocene derivatives and neridronate were successfully synthesized and characterized by NMR, FTIR, SEM, and EDX analyses. Appearance of characteristic peaks in H-1 and P-31 NMR or EDX spectra were used to confirm the presence of neridronate or ferrocene in the conjugates and co-conjugates. In vitro evaluation of the new materials revealed improved antimalarial activity, especially for conjugate 5 and corresponding co- conjugate 8, when compared with chloroquine and quinine. Hemolysis studies revealed that synthesized prodrugs had no effect on the integrity of the host red blood cell membrane; a direct effect on the intra- erythrocytic parasite was, however, noted.