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

Scientific paper - Preliminary note / Short communication

• Title (croatian): Makromolekulski prolijekovi. XII. Konjugati primakina: Sinteza i preliminarno ispitivanje antimalarijskog djelovanja
• Author: Zrinka Rajić
• Author: Gabrijela Kos
• Author: Branka Zorc
• Author: Prati Pal Singh
• Author: Savita Singh
• Author's institution: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry)
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract (english)

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.

Abstract (croatian)

U radu je opisana sinteza, karakterizacija i ispitivanje antimalarijskog djelovanja novih konjugata primakina 5-7 s glukozaminom i dva polimera poliaspartamidnog tipa, poli/a,b-(N-2-hidroksietil-DL-aspartamidom)/ (PHEA) i poli/a,b-(N-3-hidroksipropil-DL-aspartamidom)/ (PHPA). Konjugati su se razlikovali u vrsti kovalentne veze, duljini razmaknice između polimernog nosača i ljekovite tvari, molekulskoj masi i količini vezanog lijeka. Šizontocidno djelovanje pripravljenih konjugata ispitano je na miševima inficiranim Plasmodium berghei. Polimerni konjugati pokazali su jače antimalarijsko djelovanje nego konjugat s glukozaminom

• Keywords (english): primaquine; polymer-drug conjugate; polyaspartamide; glucosamine; antimalarial activity
• Keywords (croatian): primakin; polimer-lijek konjugat; poliaspartamid; glukosamin; antimalarijsko djelovanje
• Language: english
• Publication type: Scientific paper - Preliminary note / Short communication
• Publication status: Published
• Peer review: Peer review - international
• Publication version: Published version
• Journal title: Acta Pharmaceutica
• Numbering: vol. 59, no. 1, pp. 107-115
• p-ISSN: 1330-0075
• e-ISSN: 1846-9558
• DOI: https://doi.org/10.2478/v10007-009-007-x
• URN:NBN: urn:nbn:hr:163:263216
• Publication: 2009-03-01
• Document URL: https://hrcak.srce.hr/31553
• Type of resource: Text
• Access conditions: Open access
• Created on: 2018-02-14 13:39:02