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 1 H and 31 P NMR or EDX spectra were used to confirm the presence of neridronate or ferrocene in the con...

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Bibliographic Details
Published inInternational journal of polymeric materials Vol. 67; no. 7; pp. 401 - 409
Main Authors Mukaya, Elie Hembe, Van Zyl, Robyn, Van Vuuren, Natasha Jansen, Yangkou Mbianda, Xavier
Format Journal Article
LanguageEnglish
Published Philadelphia Taylor & Francis 03.05.2018
Taylor & Francis Ltd
Subjects
Antimalarial
Chemical compounds
Chemical synthesis
co-conjugates
Conjugates
Drugs
Erythrocytes
ferrocene
NMR
Nuclear magnetic resonance
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Summary:Polyamidoamine prodrugs containing ferrocene derivatives and neridronate were successfully synthesized and characterized by NMR, FTIR, SEM, and EDX analyses. Appearance of characteristic peaks in 1 H and 31 P 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.
ISSN:0091-4037
1563-535X
DOI:10.1080/00914037.2017.1342248