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Macromolecular Prodrugs. XII. Primaquine Conjugates: Synthesis and Preliminary Antimalarial Evaluation

Zrinka Rajić, Gabrijela Kos, Branka Zorc, Prati Pal Singh, Savita Singh

Acta Pharm. 2009 Mar;59(1):107-15.

PMID: 19304563

Abstract:

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

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP137629324 Poly (α,β-[N-(3-hydroxypropyl)-DL-aspartamide]) Poly (α,β-[N-(3-hydroxypropyl)-DL-aspartamide]) 137629-32-4 Price
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