Acta Pharm. 59 (2009) 107-115

 

full paper

Short communication

 

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

ZRINKA RAJIĆ, GABRIJELA KOS, BRANKA ZORC, PRATI PAL SINGH and SAVITA SINGH

bzbz@pharma.hr

1 Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia

2 National Institute of Pharmaceutical Education and Research, Sector-67, Phase-X
S.A.S. Nagar-160062, India

Accepted January 26, 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.

 

Keywords: primaquine, polymer-drug conjugate, polyaspartamide, glucosamine, antimalarial activity