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  • Title: Synthesis of some 4-substituted 8-amino-6-methoxyquinolines as potential antimalarials.
    Author: Carroll FI, Berrang B, Linn CP, Twine CE.
    Journal: J Med Chem; 1979 Jun; 22(6):694-9. PubMed ID: 110932.
    Abstract:
    The 4-vinyl, 4-ethyl, and three 4-[beta-(arylthio)ethyl] derivatives of primaquine and other 8-aminoquinoline antimalarial agents were prepared for antimalarial evaluation. 8-[(4'-Amino-1'-methylbutyl)amino]-4-ethyl-6-methoxyquinoline (4-ethylprimaquine), which showed activity approximately equal to that of primaquine against Plasmodia cynomolgi in Rhesus monkey, was the most active of the compounds tested. 4-Ethylprimaquine was also less toxic than primaquine, as measured in the Rane mouse screen.
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