Anti-leishmanial lepidine derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544 582, 544 586, 544 62, 544128, 544360, 544363, 514227, 514253, C07D40100, C07D27912, A61K 31435, A61K 3154

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active

046597085

ABSTRACT:
The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidine erivatives have the formula: ##STR1## wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O).sub.2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R" substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R'"; R" represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'" represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.

REFERENCES:
patent: 2508937 (1950-05-01), Campbell
patent: 3142679 (1964-07-01), Barrett et al.
patent: 4167638 (1979-09-01), Chen et al.
patent: 4209519 (1980-06-01), Kinnamon
Kinnamon, K. E., et al., Am. J. Trop. Med. Hyg. 27 (4), pp. 751-757 (1978).

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