<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>New primaquine conjugates <bold>5-7</bold> with glucosamine and two polymers of polyaspartamide type, poly[α,β-(<italic>N</italic>-2-hydroxyethyl-DL-aspartamide)] (PHEA) and poly[α,β-(<italic>N</italic>-3-hydroxypropyl-DL-aspartamide)] (PHPA), were synthesized, characterized and screened for their antimalarial activity. The conjugates differed in the type of covalent bonding, length of the spacer between the polymeric carrier and drug, molecular mass and drug-loading. Blood-schizontocidal activity of the prepared conjugates was tested against <italic>Plasmodium berghei</italic> infection in Swiss mice. Polymeric conjugates showed better antimalarial activity than the glucosamine conjugate.</p></abstract>

New primaquine conjugates 5-7 with glucosamine and two polymers of polyaspartamide type, poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)] (PHEA) and poly[α,β-(N-3-hydroxypropyl-DL-aspartamide)] (PHPA), were synthesized, characterized and screened for their antimalarial activity. The conjugates differed in the type of covalent bonding, length of the spacer between the polymeric carrier and drug, molecular mass and drug-loading. Blood-schizontocidal activity of the prepared conjugates was tested against Plasmodium berghei infection in Swiss mice. Polymeric conjugates showed better antimalarial activity than the glucosamine conjugate.

Macromolecular prodrugs. XII. Primaquine conjugates: Synthesis and preliminary antimalarial evaluation

Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb Croatia

National Institute of Pharmaceutical, Education and Research, Sector-67 Phase-X, S.A.S. Nagar-160062 India

Acta Pharmaceutica

New primaquine conjugates 5-7 with glucosamine and two polymers of polyaspartamide type, poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)] (PHEA) and...

Macromolecular prodrugs. XII. Primaquine conjugates: Synthesis and preliminary antimalarial evaluation

Publié en ligne: 20 mars 2009

Pages: 107 - 115

DOI: https://doi.org/10.2478/v10007-009-0007-x

Mots clés
primakin, polimer-lijek konjugat, poliaspartamid, glukozamin, antimalarijsko djelovanje

This content is open access.

Macromolecular prodrugs. XII. Primaquine conjugates: Synthesis and preliminary antimalarial evaluation

Publié en ligne: 20 mars 2009

Pages: 107 - 115

DOI: https://doi.org/10.2478/v10007-009-0007-x

Mots clésprimakin, polimer-lijek konjugat, poliaspartamid, glukozamin, antimalarijsko djelovanje

This content is open access.

Mots clés
primakin, polimer-lijek konjugat, poliaspartamid, glukozamin, antimalarijsko djelovanje