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  • 标题:Macromolecular prodrugs.XII.Primaquine conjugates: Synthesis and preliminary antimalarial evaluation
  • 本地全文:下载
  • 作者:ZRINKA RAJI ; GABRIJELA KOS ; BRANKA ZORC
  • 期刊名称:Acta Pharmaceutica
  • 电子版ISSN:1846-9558
  • 出版年度:2009
  • 卷号:59
  • 期号:1
  • 页码:107-115
  • DOI:10.2478/v10007-009-0007-x
  • 语种:English
  • 出版社:Sciendo
  • 摘要: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 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.
  • 关键词:primaquine;polymer-drug conjugate;polyaspartamide;glucosamine;antimalarial activity
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