5-(phenylalkoxy)primaquine compounds and their use for treatment

Details 5-(phenylalkoxy)primaquine compounds and their use for treatment 5-(phenylalkoxy)primaquine compounds and their use for treatment

1990-03-13

1990-12-25

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

576171, A61K 3147, C07D21520

Patent

active

049803603

ABSTRACT:
Improvement in the treatment of malaria has been demonstrated with 5-arylalkoxy primaquine compounds of the formula ##STR1## wherein R.sub.2 represents H or methyl, R represents an alkylene group having from about 2 to about 12 carbon atoms, R' represents a substituted or non-substituted aryl moiety, such as phenyl and napthyl, and pharmaceutically acceptable salts thereof, wherein the salt forming acid may be organic or inorganic in nature. These primaquine related compounds are effective in malarial chemotherapy, by exerting plasmodicidal activity on malarial parasites present in both the blood and formed tissues of the mammalian host. The 5-arylalkoxy primaquine compounds of the invention are at least as effective in malarial treatment as the prior art 5-alkoxy primaquine compounds, but are not as toxic as the 5-alkoxy compounds at higher dosage ranges.

REFERENCES:
patent: 1938047 (1933-12-01), Schonhofer et al.
patent: 2477479 (1949-07-01), Elderfield et al.
patent: 3948920 (1976-04-01), Nabih
patent: 4167638 (1979-09-01), Chen et al.
patent: 4209519 (1980-06-01), Kinnamon
patent: 4431807 (1984-02-01), Strube et al.
patent: 4554279 (1985-11-01), Saggiomo et al.

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