Peptide derivatives of primaquine as potential antimalarial agents.
Three peptide derivatives of primaquine were synthesized. The compounds were tested for radical curative antimalarial activity against Plasmodium cynomolgi in rhesus monkeys and blood schizonticidal antimalarial activity against Plasmodium berghei in mice. All three peptide derivatives showed activity against P. cynomolgi greater than that expected for the primaquine content of each prodrug. The toxicity of one of the peptide derivatives was less than that of primaquine in mice.
Philip
A
A
Research Triangle Institute, Research Triangle Park, North Carolina 27709.
Kepler
J A
JA
Johnson
B H
BH
Carroll
F I
FI
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis*; D008253:Macaca mulatta; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D010962:Plasmodium berghei; D011319:Primaquine / Q000031:analogs & derivatives* / Q000627:therapeutic use
D000962:Antimalarials; D011319:Primaquine