作为潜在抗疟药的伯氨喹肽衍生物。
Peptide derivatives of primaquine as potential antimalarial agents.
作者信息
Philip A, Kepler J A, Johnson B H, Carroll F I
机构信息
Research Triangle Institute, Research Triangle Park, North Carolina 27709.
出版信息
J Med Chem. 1988 Apr;31(4):870-4. doi: 10.1021/jm00399a032.
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.
合成了三种伯氨喹肽衍生物。对这些化合物进行了测试，以检测其对恒河猴体内食蟹猴疟原虫的根治性抗疟活性以及对小鼠体内伯氏疟原虫的血裂殖体杀灭抗疟活性。所有三种肽衍生物对食蟹猴疟原虫的活性均高于每种前药中伯氨喹含量所预期的活性。其中一种肽衍生物在小鼠中的毒性低于伯氨喹。
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