Polymeric prodrugs containing neridronate and ferrocene: Synthesis,characterization, and antimalarial activity |
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| Authors: | Elie Hembe Mukaya Robyn Van Zyl Natasha Jansen Van Vuuren |
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| Affiliation: | 1. Department of Applied Chemistry, University of Johannesburg, Doornfontein Campus, Johannesburg, Republic of South Africa;2. Pharmacology Division, Department of Pharmacy and Pharmacology;3. WITS Institute for Malaria (WRIM), Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa |
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| Abstract: | Polyamidoamine prodrugs containing ferrocene derivatives and neridronate were successfully synthesized and characterized by NMR, FTIR, SEM, and EDX analyses. Appearance of characteristic peaks in 1H and 31P 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. |
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| Keywords: | Antimalarial co-conjugates conjugates ferrocene |
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