Macromolecular prodrugs. XII. Primaquine conjugates: Synthesis and preliminary antimalarial evaluationReport as inadecuate




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Acta Pharmaceutica, Vol.59 No.1 March 2009. -

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.

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



Author: ZRINKA RAJIĆ - ; Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia GABRIJELA KOS - ; Faculty of

Source: http://hrcak.srce.hr/



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