Short communication, Note

https://doi.org/10.2478/v10007-009-007-x

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

ZRINKA RAJIĆ ; Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia
GABRIJELA KOS ; Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia
BRANKA ZORC orcid.org/0000-0003-4355-8816 ; Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia
PRATI PAL SINGH ; National Institute of Pharmaceutical Education and Research, Sector-67, Phase-X, S.A.S. Nagar-160062, India
SAVITA SINGH ; National Institute of Pharmaceutical Education and Research, Sector-67, Phase-X, S.A.S. Nagar-160062, India

Abstract

New primaquine conjugates 5-7 with glucosamine and two polymers of polyaspartamide type, poly/a,b-(N-2-hydroxyethyl-DL-aspartamide)/ (PHEA) and poly/a,b-(N-3-hydroxypropyl-DL-aspartamide)/ (PHPA), were synthesized, characterized and screened for their antimalarial activity. The conjugates differed in type of covalent bounding, length of 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. The polymeric conjugates showed better antimalarial activity than glucosamine conjugate.

Keywords

primaquine; polymer-drug conjugate; polyaspartamide; glucosamine; antimalarial activity

Hrčak ID:

31553

URI

https://hrcak.srce.hr/31553

Publication date:

1.3.2009.

Article data in other languages: croatian

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