4-methyl-5-(unsubstituted and substituted phenoxy)-2,6-dimethoxy

Details 4-methyl-5-(unsubstituted and substituted phenoxy)-2,6-dimethoxy 4-methyl-5-(unsubstituted and substituted phenoxy)-2,6-dimethoxy

1985-10-15

1986-10-14

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546153, C07D21522, A61K 3147

Patent

active

046173943

ABSTRACT:
Compounds of the class including 4-methyl-5-(unsubstituted and substituted phenoxy)-2,6-dimethoxy-8-(aminoalkylamino)quinolines as the free bases and pharmaceutically acceptable acid amine salts are described. The compounds are highly effective antimalarial agents which possess both tissue schizonticidal (radical curative) and blood schizonticidal (suppressive) acitivity. In addition, these drugs have significantly better therapeutic indices than primaquine which is the current tissue schizonticidal drug of choice. Primaquine possesses no useful blood schizonticidal activity at tolerated dose levels. The new 2-methoxy substituted compounds produce markedly less methemoglobin at effective dose levels and thus permit a higher degree of safety than analogs which are unsubstituted in the 2-position.

REFERENCES:
patent: 4431807 (1984-02-01), Struve
Mislow, Journal of the American Chemical Society, vol. 68, pp. 1553-1556, 946).
Chen, Journal of Medicinal Chemistry, vol. 20, pp. 1107-1109, (1977).

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