Synthesis of some 4-substituted 8-amino-6-methoxyquinolines as potential antimalarials

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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''-methylburyl)amino]-4-ethyl-6-methoxyquinoline (4-ethylprimaquine), which showed activity approximately equal to that of primaquine against Plasmodium 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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