4-Methyl-5-(unsubstituted and substituted phenoxy)-6-methoxy-8-(

Details 4-Methyl-5-(unsubstituted and substituted phenoxy)-6-methoxy-8-( 4-Methyl-5-(unsubstituted and substituted phenoxy)-6-methoxy-8-(

1981-12-08

1984-02-14

Coughlan, Jr., Paul M.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

424258, C07D21520, A61K 3147

Patent

active

044318073

ABSTRACT:
Compounds of the class including 4-methyl-5-(unsubstituted and substituted henoxy)-6-methoxy-8-(aminoalkylamino)quinolines as the free bases and pharmaceutically acceptable acid amine salts are described. The compounds are highly effective antimalarial agents which possess, surprisingly, both tissue schizonticidal (radical curative) and blood schizonticidal (suppressive) activity. In addition, these drugs have significantly better therapeutics indices than primaquine which is the current tissue schizonticidal drug of choice. Primaquine possesses no useful blood schizonticidal activity at tolerated dose levels.

REFERENCES:
patent: 4209519 (1980-06-01), Kinnaman
Chen et al., J. Med. Chem 20, pp. 1107-1109, (1971).
La Mantagne et al., J. Med. Chem, 20, pp. 1122-1127, (1977).

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