Macromolecular prodrugs. XII. Primaquine conjugates: synthesis and preliminary antimalarial evaluation.
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.
Rajić
Zrinka
Z
Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb Croatia.
Kos
Gabrijela
G
Zorc
Branka
B
Singh
Prati Pal
PP
Singh
Savita
S
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D005944:Glucosamine / Q000737:chemistry; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D008297:Male; D051379:Mice; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D010962:Plasmodium berghei / Q000187:drug effects; D011319:Primaquine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D004337:Drug Carriers; D010455:Peptides; D011355:Prodrugs; C008965:alpha,beta-poly((2-hydroxyethyl)-aspartamide); D011319:Primaquine; D005944:Glucosamine